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alpha4beta2

" in MedChemExpress (MCE) Product Catalog:

88

Inhibitors & Agonists

1

Biochemical Assay Reagents

2

Peptides

9

Natural
Products

7

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108069

    Potassium Channel nAChR Neurological Disease
    Iptakalim hydrochloride, a lipophilic para-amino compound, is a novel ATP-sensitive potassium channel (KATP) opener, as well as an α4β2-containing nicotinic acetylcholine receptor (nAChR) antagonist .
    Iptakalim hydrochloride
  • HY-110160

    ABT-089 dihydrochloride

    nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites . Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant .
    Pozanicline dihydrochloride
  • HY-103066

    nAChR Neurological Disease
    Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
    Br-PBTC
  • HY-107675

    Deformylflustrabromine hydrochloride; dFBr hydrochloride

    nAChR Neurological Disease
    Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
    Desformylflustrabromine hydrochloride
  • HY-115764

    nAChR Neurological Disease
    nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM) .
    nAChR agonist 2
  • HY-N1064

    nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2) .
    Xanthoplanine
  • HY-110142

    CC4

    nAChR Neurological Disease
    Thermopsidine (CC4) is a selective partial agonist at α4β2/α6β2 nAChR with EC50 values of 2.2 μM target α4β2 .
    Thermopsidine
  • HY-116149

    nAChR Others
    A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
    A-424274
  • HY-107673

    nAChR Neurological Disease
    RJR 2429 hydrochloride is a α4β2 and α7 nAChR agonist .
    RJR-2429 dihydrochloride
  • HY-169870

    (+)-Mecamylamine; TC-5214

    nAChR Neurological Disease
    Dexmecamylamine ((+)-Mecamylamine) is the antagonist for nicotinic acetylcholine receptor (nAChR), that antagonises the α3β4/α4β2/α7/α1β1γδ receptor with IC50 of micromolare levels. Dexmecamylamine exhibits anxiolytic and antidepressant-like activities .
    Dexmecamylamine
  • HY-14564A
    GTS-21 dihydrochloride
    5+ Cited Publications

    DMXB-A; DMBX-anabaseine

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
    GTS-21 dihydrochloride
  • HY-10063

    TC-1734; ACD3480

    nAChR Neurological Disease
    Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
    Ispronicline
  • HY-14316A

    Ebanicline dihydrochloride; ABT-594 dihydrochloride

    nAChR Neurological Disease
    Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
    Tebanicline dihydrochloride
  • HY-14316B

    Ebanicline hydrochloride; ABT-594 hydrochloride

    nAChR Neurological Disease
    Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
    Tebanicline hydrochloride
  • HY-107677

    nAChR Neurological Disease
    A 844606 is a highly potent and selective α4β2 nAChR agonist. A 844606 can be used in the study of schizophrenia, Huntington's disease, Alzheimer's disease, and Parkinson's disease .
    A 844606
  • HY-N2326

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM) .
    (±)-Anatoxin A fumarate
  • HY-139581

    SUVN-911 free base

    nAChR Neurological Disease
    Ropanicant (SUVN-911 free base) is a novel, potent, selective, and orally active neuronal nicotinic acetylcholine α4β2 receptor antagonist for the research of depression .
    Ropanicant
  • HY-B0942S

    Isotope-Labeled Compounds nAChR Neurological Disease
    Benzethonium-d7 chloride is the deuterium labeled Benzethonium chloride. Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
    Benzethonium-d7 chloride
  • HY-107671

    nAChR Neurological Disease
    DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects .
    DMAB-anabaseine dihydrochloride
  • HY-136207

    nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
    TC-2559 difumarate
  • HY-110241

    nAChR Neurological Disease
    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .
    Dianicline dihydrochloride
  • HY-W979493

    Others Others
    TC-2216 is a compound with antidepressant and anxiolytic activity that has shown activity in multiple animal models and may exert its effects by acting on α4β2 neuronal nicotinic receptors.
    TC-2216
  • HY-110131

    nAChR Neurological Disease
    A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
    A 85380 hydrochloride
  • HY-14312

    nAChR Neurological Disease
    A 85380 is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 exhibits selectivity for the α4β2 nAChR subtypes. A 85380 has a broad-spectrum analgesic profile .
    A85380
  • HY-10019

    CP 526555

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline
  • HY-10020

    CP 526555 hydrochloride

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Hydrochloride
  • HY-10021

    CP 526555-18

    nAChR ERK p38 MAPK Others Neurological Disease Cancer
    Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline Tartrate
  • HY-107684

    3-Br-cytisine

    nAChR Neurological Disease
    3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC50s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC50s are 8 and 50 nM, respectively .
    3-Bromocytisine
  • HY-10019A

    CP 526555 dihydrochloride

    nAChR Neurological Disease Inflammation/Immunology Cancer
    Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline dihydrochloride
  • HY-14564

    nAChR 5-HT Receptor Inflammation/Immunology
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist. GTS-21 can be used in age-associated memory impairment (AAMI) and Alzheimer's disease research .
    GTS-21
  • HY-136146

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity .
    SUVN-911
  • HY-136947

    nAChR Neurological Disease
    RJR-2429 is a nAChR agonist (EC50: 59 nM). RJR-2429 binds with high affinity to α4β2 receptor subtype (Ki = 1 nM). RJR-2429 induces ileum contraction .
    RJR-2429
  • HY-138879A

    nAChR Neurological Disease
    (Rac)-CP-601927 hydrochloride is the racemate of CP-601927. CP-601927 is a nAChR agonist with Ki values 1.2 nM and 102 nM for α4β2 and α3β4 nAChR, respectively .
    (Rac)-CP-601927 hydrochloride
  • HY-107680

    3-Pyr-Cyt

    nAChR Neurological Disease
    3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant .
    3-Pyr-Cytisine
  • HY-107686

    5-I A-85380 dihydrochloride

    nAChR Neurological Disease
    5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively .
    5-Iodo-A-85380 dihydrochloride
  • HY-14316

    Ebanicline; ABT-594

    nAChR Neurological Disease
    Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
    Tebanicline
  • HY-B0942R

    nAChR Bacterial Neurological Disease
    Benzethonium (chloride) (Standard) is the analytical standard of Benzethonium (chloride). This product is intended for research and analytical applications. Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.
    Benzethonium (chloride) (Standard)
  • HY-14316C

    Ebanicline tosylate; ABT-594 tosylate

    nAChR Neurological Disease
    Tebanicline tosylate, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline tosylate exhibits potent antinociceptive effects and has a high affinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
    Tebanicline tosylate
  • HY-13225D

    RJR-2403 fumarate; (E)-Metanicotine fumarate

    nAChR Neurological Disease
    Rivanicline fumarate is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .
    Rivanicline fumarate
  • HY-120946

    nAChR Neurological Disease
    VMY-2-95 is an oral active and blood-brain barrier (BBB) penetrant α4β2 nicotinic acetylcholine receptor desensitizer. VMY-2-95 can be used for study of depression or addiction .
    VMY-2-95
  • HY-12766

    Dopamine Transporter nAChR Neurological Disease
    Bupropion morpholinol (Hydroxy Bupropion) is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
    Bupropion morpholinol
  • HY-40421

    Biochemical Assay Reagents Others
    (R)-3-Fluoropyrrolidine hydrochloride is a derivative of fluorinated pyrrolidines. The amide series of fluorinated pyrrolidines are inhibitors of dipeptidyl peptidase DP-IV. Novel α4β2 receptor ligands characterized by a 3-Fluoropyrrolidine core .
    (R)-3-Fluoropyrrolidine hydrochloride
  • HY-115766

    nAChR Neurological Disease
    Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
    Anabaseine
  • HY-138953

    nAChR Neurological Disease
    Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .
    Epiboxidine
  • HY-138953A

    nAChR Neurological Disease
    Epiboxidine hydrochloride is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine hydrochloride is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418 .
    Epiboxidine hydrochloride
  • HY-10021R

    nAChR ERK p38 MAPK Others Neurological Disease
    Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
    Varenicline (Tartrate) (Standard)
  • HY-13225A

    RJR-2403; (E)-Metanicotine

    nAChR Neurological Disease
    Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype,Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor .
    Rivanicline
  • HY-N0175
    Cytisinicline
    1 Publications Verification

    Cytisine; Sophorine; Baptitoxine

    nAChR Metabolic Disease Cancer
    Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
    Cytisinicline
  • HY-12766S

    Isotope-Labeled Compounds nAChR Dopamine Transporter Neurological Disease
    Bupropion morpholinol-d6 is the deuterated form of Bupropion morpholinol. Bupropion morpholinol is a major metabolite of Bupropion. Bupropion morpholinol inhibits Dopamine, Norepinephrine transporters and the α4β2 nicotinic receptor in vitro. Bupropion morpholinol contributes to antidepressant and smoking cessation activities .
    Bupropion morpholinol-d6
  • HY-13225

    RJR-2403 oxalate; (E)-Metanicotine oxalate

    nAChR Neurological Disease
    Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
    Rivanicline oxalate

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