From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
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 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 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 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 .
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 .
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 .
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 .
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 .
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.
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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].
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 .
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 a tritiated version 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 .
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 .
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 .
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.
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.
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 .
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 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 .
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 .
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 .
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 .
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 .
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 .
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.
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 .
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 .
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 .
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 .
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 .
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) .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
[(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) .
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 .
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 .
MOR agonist-3 (Compound 84) is a D3R/MOR antagonist (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 .
(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 .
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 .
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 .
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 .
(-)-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) .
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 .
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.
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.
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 .
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 .
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 .
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 .
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) .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
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 .
[(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) .
(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 .
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 .
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 .
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 .
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 (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.
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].
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 a tritiated version 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 .
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 .
Inquiry Online
Your information is safe with us. * Required Fields.
![[(pF)Phe4]Nociceptin(1-13)NH2](http://file.medchemexpress.eu/product_pic/hy-p1300.gif)
![[(pF)Phe4]Nociceptin(1-13)NH2 TFA](http://file.medchemexpress.eu/product_pic/hy-p1300a.gif)
