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Acetylcholine Nicotinic Receptors
Nicotinic receptors (nAChRs) are ligand-gated ion channels that modulate cell membrane potentials. Each receptor is composed of pentameric combinati*** of subunits (α1-10, β1-4, δ, ε and γ). Nicotinic receptors are generally divided into three functional classes: muscle subunits (α1, β1, δ, ε, γ), standard neuronal subunits (α1-6 and β2-4) that form in pairwise αβ combinati***, and subunits (α7-9) that can form homomeric nAChRs. Neuronal nicotinic receptors are found in the central nervous system and in autonomic ganglia where they regulate processes such as tran***itter release, cell excitability and neuronal integration. Nicotinic receptors located at the neuromuscular juncti*** of somatic muscles are resp***ible for muscular contraction.
Nicotinic (α4β2) Receptor Products
3549 3-Bromocytisine
Potent agonist of α4β4, α4β2 and α7 nACh receptors
1518 5-Iodo-A-85380 dihydrochloride
High affinity α4β2 and α6β2 subtype-selective agonist
1527 5-Iodo-A-85380, 5-trimethylstannyl N-BOC derivative
Precursor to 5-Iodo-A-85380 (Cat. No. 1518)
3546 (-)-Nicotine ditartrate
α4β2 agonist
1053 RJR 2403 oxalate
α4β2 selective nicotinic agonist
2737 TC 2559 difumarate
Selective partial agonist at α4β2 receptors
3754 Varenicline tartrate
Orally active, subtype-selective α4β2 partial agonist
Antagonists
2349 Dihydro-β-erythroidine hydrobromide
Antagonist for neuronal α4-containing nicotinic receptors
2241 DMAB-anabaseine dihydrochloride
Antagonist at α4β2 receptors and partial agonist at α7-containing neuronal nicotinic receptors
Modulators
3328 Desformylflustrabromine hydrochloride
Positive allosteric modulator of α4β2
4141 LY 2087101
Potentiator of α4β2 nAChRs
Other
4125 3-pyr-Cytisine
High affinity, partial agonist of α4β2 receptors
2736 Sazetidine A dihydrochloride
α4β2 receptor ligand; may act as an agonist or a desensitizer
Nicotinic (α7) Receptor Products
Agonists
3549 3-Bromocytisine
Potent agonist of α4β4, α4β2 and α7 nACh receptors
2241 DMAB-anabaseine dihydrochloride
Partial agonist at α7-containing receptors and antagonist at α4β2 neuronal nicotinic receptors
3092 PHA 543613 hydrochloride
Potent and selective α7 nAChR agonist
3134 PHA 568487
α7-selective agonist
2303 PNU 282987
Selective α7 nAChR agonist
3518 S 24795
Partial agonist at α7 nAChR
2518 TC 1698 dihydrochloride
α7-selective agonist
Antagonists
2133 α-Bungarotoxin
α7 subtype-selective nAChR antagonist
3405 COG 133
apoE peptide fragment; α7 nAChR antagonist
3119 α-Conotoxin ImI
α7 and α9 selective nAChR antagonist
1029 Methyllycaconitine citrate
α7 neuronal nicotinic receptor antagonist
1356 MG 624
α7 neuronal nicotinic receptor antagonist
Modulators
3837 CCMI
Positive allosteric modulator of α7 nAChR
1260 Ivermectin
Allosteric modulator of α7 nicotinic receptors
4141 LY 2087101
Potentiator of α7 nAChRs
2995 NS 1738
Positive allosteric modulator of α7 nAChR; active in vivo
2498 PNU 120596
Positive allosteric modulator of α7 nAChR; active in vivo
4233 TQS
Positive allosteric modulator of α7 nAChRs
Other
3091 FR 236924
Enhances α7 nAChR activity; PKCε activator
Purity: >99 % 10mg
Nicotinic Receptor (Non-Selective) Products
Agonists
2809 Acetylcholine chloride
Endogenous neurotran***itter
0352 4-Acetyl-1,1-dimethylpiperazinium iodide
Nicotinic agonist
0351 1-Acetyl-4-methylpiperazine hydrochloride
Nicotinic agonist
1971 (+)-Anabasine hydrochloride
Neuronal nicotinic receptor agonist
0789 (&plu***n;)-Anatoxin A fumarate
Nicotinic agonist
3549 3-Bromocytisine
Potent agonist of α4β4, α4β2 and α7 nACh receptors
2810 Carbamoylcholine chloride
Cholinergic receptor agonist
3110 (-)-Cotinine
Major metabolite of nicotine
1390 (-)-Cytisine
Potent, selective neuronal nicotinic agonist
0684 (&plu***n;)-Epibatidine
Very potent nicotinic agonist
1077 (-)-Lobeline hydrochloride
Nicotinic agonist
1271 RJR 2429 dihydrochloride
Nicotinic receptor agonist
Antagonists
0424 Benzoquinonium dibromide
Nicotinic antagonist
2722 Catestatin
Non-competitive nicotinic cholinergic antagonist
1001 Chlorisondamine diiodide
Nicotinic antagonist; slow offset
2843 Mecamylamine hydrochloride
Non-competitive nicotinic receptor antagonist
0693 Pancuronium dibromide
Nicotinic (neuromuscular) antagonist
2785 *** hydrochloride
Nicotinic receptor antagonist
2438 TMPH hydrochloride
Neuronal nicotinic receptor antagonist
2820 (+)-Tubocurarine chloride pentahydrate
Nicotinic receptor antagonist
Blockers
4111 Hexamethonium bromide
Nicotinic receptor blocker
Nicotinic Receptor (Other Subtype) Products
Agonists
3549 3-Bromocytisine
Potent agonist of α4β4, α4β2 and α7 nACh receptors
1518 5-Iodo-A-85380 dihydrochloride
High affinity α4β2 and α6β2 subtype-selective agonist
1527 5-Iodo-A-85380, 5-trimethylstannyl N-BOC derivative
Precursor to 5-Iodo-A-85380 (Cat. No. 1518)
1348 UB 165 fumarate
Subunit selective nAChR agonist
Antagonists
3205 ACV 1
α9α10-selective antagonist
3120 α-Conotoxin AuIB
Selective α3β4 nAChR antagonist
3124 α-Conotoxin EI
α1β1δγ selective nAChR antagonist
3119 α-Conotoxin ImI
α7 and α9 selective nAChR antagonist
1340 α-Conotoxin MII
Potent α3β2 and β3 subunit selective nicotinic antagonist
3121 α-Conotoxin PIA
Selective antagonist of α6-containing nicotinic receptors
3123 α-Conotoxin PnIA
Selective α3β2 nAChR antagonist
2349 Dihydro-β-erythroidine hydrobromide
Antagonist for neuronal α4-containing nicotinic receptors
Modulators
4141 LY 2087101
Potentiator of nAChRs
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