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μ opioidreceptor agonist 3 (compound 20) is a potent μ opioidreceptor (µOR) agonist with an EC50 of 0.87 nM. μ opioidreceptor agonist 3 has the potential for pain and neuropsychiatric indications research .
μ opioidreceptor agonist 2 （Compound H-3）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MORreceptor agonist and can be used for the research of pain and pain related diseases .
μ opioidreceptor agonist 1 （Compound H-1a）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MORreceptor agonist and can be used for the research of pain and pain related diseases .
Mu opioidreceptor antagonist 8 (368) is a μ-opioidreceptor antagonist. Mu opioidreceptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
Mu opioidreceptor antagonist 4 (compound 31) is a potent and selective μ opioidreceptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioidreceptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioidreceptor antagonist 4 Mu opioidreceptor antagonist 4 can be used for researching opioid use disorders (OUD) .
Mu opioidreceptor antagonist 3 (compound 26) is a potent and selective μ opioidreceptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioidreceptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioidreceptor antagonist 3 can be used for researching opioid use disorders (OUD) .
Mu opioidreceptor antagonist 1 (compound 19) is a selective and orally active μ opioidreceptor (MOR) ligand with an Ki value of 0.58 nM and an EC50 of 1.15 nM. Orally administrating with Mu opioidreceptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioidreceptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .
Mu opioidreceptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioidreceptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioidreceptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioidreceptor antagonist 2 can be used for researching opioid use disorders (OUD) .
Mu opioidreceptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioidreceptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioidreceptor antagonist 5 can be used for researching opioid use disorders (OUD) .
Mu opioidreceptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioidreceptor), with an IC50 of 29 ± 3.0 nM. Mu opioidreceptor antagonist 7 can be used for the research of pain and opioid use disorder .
σ1 Receptor/μ Opioidreceptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioidreceptor agonist with Kis of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioidreceptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioidreceptor modulator 1 can be used for the research of neuropathic pain .
3-Carboxamidonaltrexone (example 32) is a opioidreceptor binding compound with Ki values of 1.9 nM, 110 nM, and 22 nM for μ-opioidreceptor, δ-opioidreceptor, and K-opioidreceptor, respectively .
MOR agonist-1 is a MOR (μ-opioidreceptor) agonist. MOR agonist-1 has good analgesic effect. MOR agonist-1 can be used for the research of pain and pain-related disorders .
(-)-9-Hydroxycorynantheidine (9-O-Desmethyl mitragynine), the 9-demethyl analogue of Mitragynine, is a selective and partial agonist of μ-opioidreceptor. (-)-9-Hydroxycorynantheidine inhibits electrically stimulated twitch contraction in guinea-pig ileum .
CTOP is a potent and highly selective μ-opioidreceptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioidreceptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan hydrochloride primarily acts as an opioidreceptor antagonist in vivo .
Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioidreceptors. Samidorphan acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan primarily acts as an opioidreceptor antagonist in vivo .
Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus .
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .
SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioidreceptor partial agonist, with high binding affinity (NOP receptorKi=7.49; μ-OpioidreceptorKi=2.70). SR-16435 can relieve pain .
DALDA acetate is a potent and highly selective μ-opioidreceptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioidreceptors. Samidorphan acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan primarily acts as an opioidreceptor antagonist in vivo .
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioidreceptors. Samidorphan is a μ-opioidreceptor antagonist and a partial agonist at k-opioid and δ-opioidreceptors. Samidorphan acts primarily as an opioidreceptor antagonist in vivo .
Naloxonazine dihydrochloride is a specific μ-opioidreceptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity .
Naldemedine (S-297995) tosylate is an orally active μ-opioidreceptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioidreceptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
Naldemedine (S-297995) is an orally active μ-opioidreceptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC50=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioidreceptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
GSK1521498 is a potent and selective μ-opioidreceptor (MOR) antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents .
Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation[1][2].
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
TAN-452 is an orally active, selective peripherally acting δ-opioidreceptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioidreceptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioidreceptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
AP-238 is a a new synthetic opioid (NSO), and acts as an agonist for μ-opioidreceptor (MOR) with an EC50 of 248 nM. AP-238 exhibits analgesic activity .
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
GSK1521498 free base is a potent and selective μ-opioidreceptor (MOR) antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents .
CTAP is a potent, highly selective, and BBB penetrant μ opioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
Cyprodime hydrochloride is a highly selective μ-opioidreceptor antagonist with Ki values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioidreceptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect .
GSK1521498 free base (hydrochloride) is a potent and selective μ-opioidreceptor (MOR) antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents .
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioidreceptor via an endorphin-like pathway .
CYM51010 is a biased ligand of μ-opioidreceptor – δ-opioidreceptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .
Bromadoline maleate is an opioid analgesic selective for the μ-opioidreceptor, exhibiting analgesic activity in various biological fluids. Bromadoline maleate has been successfully quantified alongside its N-demethylated metabolites in human and canine samples.
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioidreceptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioidreceptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM) .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Isotodesnitazene is a kind of opioids. Isotodesnitazene primarily acts on μ-opioidreceptors (MOR). Isotodesnitazene has an EC50 of 34.8 nM for MOR-βarr2 and 142 nM for MOR-mini-Gi. Isotodesnitazene can be used in the study of opioids .
Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-OpioidReceptor (MOPr) agonist (Ki=210 nM, hMOPr) .
Fluorphine is an analogue of Brorphine and can bind to μ-opioidreceptor (MOR) (Ki: 12.5 nM). Fluorphine has GTPγS binding (EC50: 75 nM) and βarrestin 2 recruitment (EC50: 377 nM) activity. Fluorphine induces respiratory depressant effects .
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioidreceptor, with analgesic effect .
Atoxifent is a potent μ-opioidreceptor agonist (EC50=0.39 nM). These receptors are found in brain regions that control pain, emotions, habitual learning, and cognition. Atoxifent exhibits strong analgesic effects and a lower risk of respiratory depression. Atoxifent can be used for research in opioid pharmacology and signal transduction .
EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioidreceptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity .
α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioidreceptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling .
Biocytin-β-endorphin, human is abiotinylated β-Endorphin, human (HY-P1502). β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
EST73502 monohydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioidreceptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 monohydrochloride has antinociceptive activity .
β-Endorphin, an endogenous opioid neuropeptide, is an opioidreceptor agonist. β-Endorphin binds preferentially to μ-opioidreceptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
(±)-Salsolinol hydrochloride is the hydrochloride form of (±)-Salsolinol (HY-113316). (±)-Salsolinol hydrochloride is a Dopamine (HY-B0451)-derived endogenous metabolite. (±)-Salsolinol hydrochloride activates μ-opioidreceptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA) .
O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioidreceptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
NAQ is a potent and selective μ opioidreceptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioidreceptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
CP-866,087 is a novel, potent and selective μ-opioidreceptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioidreceptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
Alvimopan metabolite is a μ opioidreceptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioidreceptor antagonist during research and development .
PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioidreceptors(µ-opioidreceptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
(RS)-Salsolinol hydrobromide is the hydrobromide form of (±)-Salsolinol (HY-113316). (RS)-Salsolinol hydrobromide is a Dopamine (HY-B0451)-derived endogenous metabolite. (RS)-Salsolinol hydrobromide activates μ-opioidreceptors (MORs), reduces GABAergic transmission, increases the excitability of dopamine (DA) neurons, and thus accelerates the sustained firing of neurons in the posterior ventral tegmental area (pVTA) .
Corydaline (Standard) is the analytical standard of Corydaline. This product is intended for research and analytical applications. Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioidreceptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
BPRMU191 is a μ-opioidreceptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .
(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioidreceptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs .
MOR agonist-3 (Compound 84) is a D3R/MOR antagonist/partial agonist a(Ki 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioidreceptor) (HY-149337) partial agonists and to reduce opioid abuse through D3R antagonists. MOR agonist-3 can be used in the treatment of inflammation and neuropathic pain research .
Methyl-6-alpha-Naltrexol is a metabolite of Methylnaltrexone (MNTX). Methylnaltrexone is a selective mu-opioidreceptor antagonist and functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract .
Loperamide (ADL 2-1294) is a selective μ opioidreceptor agonist with Kis of 3, 48 and 1156 nM against μ, δ and κ opioidreceptor, respectively. Loperamide can be used as an antidiarrheal agent .
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioidreceptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs .
Valorphin is an endogenous hemoglobin β-chain (33-39) fragment with opioid analgesic activity, binds to rat mu-opioidreceptor, with an IC50 of 14 nM; Valorphin also shows anti-tumor activity.
AT-121 is a bifunctional nociception and mu opioidreceptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects .
AT-121 hydrochloride is a bifunctional nociception and mu opioidreceptor agonist, with Kis of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects .
μ/κ/δ opioidreceptor agonist 1 is a μ opioidreceptor (MOR), κ opioidreceptor (KOR), and δ opioidreceptor (DOR) agonist. μ/κ/δ opioidreceptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
CYT-1010 hydrochloride is a mu-opioidreceptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .
CYT-1010 is a mu-opioidreceptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .
PL-017 is a potent and selective μ opioidreceptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
PL-017 TFA is a potent and selective μ opioidreceptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
BPR1M97 is a dual-acting mu opioidreceptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with Ki values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects .
RO-76 is a mu opioidreceptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC50 value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioidreceptors (>3000 fold) .
[(pF)Phe4]Nociceptin(1-13)NH2 TFA is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 TFA displays high selectivity over δ, κ, and μ opioidreceptors (>3000 fold) .
MOR modulator-1 (compound 6) is a potent and selective μ opioidreceptor (MOR) modulator. MOR modulator-1 exhibits improved opioidreceptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with Ki of 0.25, 41.1, 1.30 nM, respectively[1]
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioidreceptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioidreceptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
BU09059 is a potent and selective Kappa-opioidreceptor antagonist with a pA2 of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .
Piperidylthiambutene is a potent µ-opioidreceptor (MOR) agonist with a Ki of 2.75 nM. Piperidylthiambutene exhibits analgesic and antitussive properties and can be utilized in relevant research .
N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioidreceptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
CP-96021 is a potent and orally available leukotriene D4 (LTD4Ki=34 μM) / platelet activating factor (PAFKi=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and GABAreceptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma .
CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioidreceptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure .
CTOP is a potent and highly selective μ-opioidreceptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .
DALDA acetate is a potent and highly selective μ-opioidreceptor agonist with a Ki of 1.69 nM. DALDA acetate shows antinociceptive and respiratory effects .
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioidreceptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
CTAP is a potent, highly selective, and BBB penetrant μ opioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
Acetyl tetrapeptide-15 is a synthetic peptide used in the cosmetics for sensitive skin. Acetyl tetrapeptide-15 is derived from endomorphin-2 (Tyr-Pro-Phe-Phe-NH2), a human μ-opioid agonist with selective anti-nociceptive effect. Acetyl tetrapeptide-15 reduces skin hyperreactivity producing inflammatory, chronic and neuropathic pain, by increasing the threshold of neuronal excitability in μ-opioidreceptor via an endorphin-like pathway .
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioidreceptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-OpioidReceptor (MOPr) agonist (Ki=210 nM, hMOPr) .
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioidreceptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling .
Biocytin-β-endorphin, human is abiotinylated β-Endorphin, human (HY-P1502). β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioidreceptor, with preferred affinity for μ-opioidreceptor and δ-opioidreceptor; β-Endorphin, human exhibits antinociception activity.
β-Endorphin, an endogenous opioid neuropeptide, is an opioidreceptor agonist. β-Endorphin binds preferentially to μ-opioidreceptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioidreceptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs .
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioidreceptor antagonist with high affinity for μ and κ3 opioidreceptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
μ/κ/δ opioidreceptor agonist 1 is a μ opioidreceptor (MOR), κ opioidreceptor (KOR), and δ opioidreceptor (DOR) agonist. μ/κ/δ opioidreceptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .
PL-017 is a potent and selective μ opioidreceptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
PL-017 TFA is a potent and selective μ opioidreceptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
[(pF)Phe4]Nociceptin(1-13)NH2 is a highly potent and selective NOP receptor (OP4) agonist, with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 displays high selectivity over δ, κ, and μ opioidreceptors (>3000 fold) .
Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioidreceptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioidreceptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioidreceptor (Ki=0.47 nM) over κ- and δ-opioidreceptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .
Sinomenine (Standard) is the analytical standard of Sinomenine. This product is intended for research and analytical applications. Sinomenine, an alkaloid extracted from?Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation . Sinomenine also is an activator of μ-opioidreceptor .
Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioidreceptor, with analgesic effect .
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioidreceptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
Corydaline (Standard) is the analytical standard of Corydaline. This product is intended for research and analytical applications. Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 μM. Corydaline is a μ-opioidreceptor (Ki of 1.23 μM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 μM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities .
The OPRM1 protein serves as a receptor for endogenous and synthetic opioids and undergoes conformational changes upon agonist binding, activating downstream signaling pathways. This includes coupling to G proteins, thereby regulating adenylyl cyclase, calcium channels, potassium channels, and intracellular signaling pathways. OPRM1 Protein, Human (Cell-Free, His) is the recombinant human-derived OPRM1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of OPRM1 Protein, Human (Cell-Free, His) is 400 a.a., with molecular weight of 47.6 kDa.
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioidreceptors. Samidorphan acts as an antagonist at μ‐opioidreceptors and acts as a partial agonist at k-opioid and δ‐opioidreceptors. Samidorphan primarily acts as an opioidreceptor antagonist in vivo .
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioidreceptors. Samidorphan is a μ-opioidreceptor antagonist and a partial agonist at k-opioid and δ-opioidreceptors. Samidorphan acts primarily as an opioidreceptor antagonist in vivo .
Naloxegol-d5 (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioidreceptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation[1][2].
O-Desmethyltramadol-d6 (hydrochloride) is a deuterated labeled O-Desmethyltramadol (hydrochloride) . O-Desmethyltramadol (hydrochloride) is a primary active metabolite of Tramadol. O-Demethyltramadol is mainly responsible for its μ-opioidreceptor-related analgesic effect. Tramadol is metabolized to O-Demethyltramadol mainly by the cytochrome P450 (CYP) 2D6 enzyme .
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