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Home , Decamethonium, Encenicline, Epibatidine, Rivanicline, Tebanicline, Varenicline

nAChR Nicotinic receptors

nAChRs (nicotinic acetylcholine receptors) are neuron receptor proteins that signal for muscular contraction upon a chemical stimulus. They are receptors that form -gated ion channels in the plasma membranes of certain neurons and on the presynaptic and postsynaptic sides of theneuromuscular junction. Nicotinic acetylcholine receptors are the best-studied of the ionotropic receptors. Like the other type of -the muscarinic acetylcholine receptor (mAChR)-the nAChR is triggered by the binding of the acetylcholine (ACh). Just as muscarinic receptors are named such because they are also activated by , nicotinic receptors can be opened not only by acetylcholine but also by —hence the name "nicotinic".

www.MedChemExpress.com 1 nAChR Inhibitors & Modulators

(+)-Sparteine (-)-(S)-B-973B Cat. No.: HY-W008350 Cat. No.: HY-114269

Bioactivity: (+)-Sparteine is a natural acting as a ganglionic Bioactivity: (-)-(S)-B-973B is a potent allosteric and positive blocking agent. (+)-Sparteine competitively blocks nicotinic allosteric modulator of α7 nAChR, with antinociceptive ACh receptor in the neurons. activity [1].

Purity: 98.0% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

(±)- A-867744 (CMI 545) Cat. No.: HY-101078 Cat. No.: HY-12149

Bioactivity: (±)-Epibatidine is a . (±)-Epibatidine is a Bioactivity: A-867744 is a positive allosteric modulator of α7 nAChRs (IC50 neuronal nAChR agonist. values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X. laevis oocytes). Displays no activity at 5-HT3A, α3β4 or α4β2 nAChRs. IC50 value: ~ 1 uM Target: α7 nAChR Target: Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Adiphenine hydrochloride Cat. No.: HY-B0379A ((S)-Anabasine) Cat. No.: HY-B1532

Bioactivity: Adiphenine HCl is a nicotinic receptor inhibitor, used as an Bioactivity: Anabasine is a nicotinic receptor agonist. antispasmodic drug.

Purity: 99.62% Purity: 98.71% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 25 mg, 50 mg, 100 mg

Aniracetam Atracurium besylate (Ro 13-5057) Cat. No.: HY-10932 (BW-33A) Cat. No.: HY-B0292A

Bioactivity: Aniracetam(Ro 13-5057) is a and neuroprotective Bioactivity: Atracurium Besylate is a neuromuscular blocking agent with drug, which is selectively modulates the AMPA receptor and ED95 of 0.2 mg/kg. Target: nAChR Atracurium besylate is a nAChR. neuromuscular-blocking drug or skeletal in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in to facilitate endotracheal… Purity: 99.43% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 50 mg, 100 mg, 500 mg

BNC375 Carbamoylcholine chloride Cat. No.: HY-128575 (; Carbamylcholine chloride) Cat. No.: HY-B1208

Bioactivity: BNC375 is a potent, selective, and orally available type I Bioactivity: Carbamoylcholine chloride is used to study responses mediated

positive allosteric modulator of α7 nAChRs with an EC50 of by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling. IC50 value: 10 to 10,000 nM 1.9 μM [1]. (Ki) Target: nAChR, mAChR Carbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR).… Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Catharanthine Cholesterol myristate ((+)-3,4-Didehydrocoronaridine) Cat. No.: HY-N0252 (Cholesteryl myristate; Cholesteryl tetradecanoate) Cat. No.: HY-N2338

Bioactivity: Catharanthine inhibits nicotinic receptor mediated diaphragm Bioactivity: Cholesterol myristate is a natural steroid present in contractions with IC50 of 59.6 μM. Target: nAChR Catharanthine traditional Chinese medicine. Cholesterol myristate binds to evokes a concentration-dependent attenuation of carbachol several ion channels such as the nicotinic acetylcholine responses in the rat ileum preparation, producing rightward receptor, GABAA receptor, and the inward-rectifier curve displacements and decreases in maximal agonist… potassium ion channel. Purity: 98.66% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg 50 mg, 100 mg

Cisatracurium besylate Cyclodrine hydrochloride (51W89) Cat. No.: HY-13596 Cat. No.: HY-U00139

Bioactivity: Cisatracurium Besylate (51W89) is a nondepolarizing Bioactivity: Cyclodrine hydrochloride is a cholinergic (muscarinic, neuromuscular blocking agent, antagonizing the action of nicotinic) ( mAChR and nAChR) . acetylcholine by inhibiting neuromuscular transmission.

Purity: 98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg, 20 mg 25 mg, 50 mg, 100 mg

Cytisinicline Bromide (; Sophorine; Baptitoxine) Cat. No.: HY-N0175 Cat. No.: HY-B0570

Bioactivity: Cytisinicline (Cytisine) is an alkaloid that occurs naturally Bioactivity: Decamethonium Bromide is a nicotinic AChR and in several genera, such as Laburnum and Cytisus. neuromuscular blocking agent. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs [1], and partial to full agonist at β4 containing recept…

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 25 mg 5 g, 10 g

Desformylflustrabromine hydrochloride Dinotefuran (Deformylflustrabromine hydrochloride; dFBr hydrochloride) Cat. No.: HY-107675 (MTI-446) Cat. No.: HY-B0827

Bioactivity: hydrochloride is a selective agonist Bioactivity: Dinotefuran is an insecticide of the neonicotinoid class, its

of α4β2 neuronal nicotinic acetylcholine receptor ( nAChR) mechanism of action involves disruption of the insect's with a pEC of 6.48. nervous system by inhibiting nicotinic acetylcholine 50 receptors. Target: nAChR, Antiparasitic

Purity: 99.77% Purity: 99.63% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 50 mg, 100 mg

Encenicline hydrochloride (EVP-6124) Cat. No.: HY-15430 (EVP-6124 (hydrochloride)) Cat. No.: HY-15430A

Bioactivity: Encenicline (EVP-6124) is a novel partial agonist of α7 Bioactivity: Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel neuronal nicotinic acetylcholine receptors ( nAChRs). partial agonist of α7 neuronal nicotinic acetylcholine receptors ( nAChRs).

Purity: >98% Purity: 98.20% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

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GTS-21 dihydrochloride Bromide (DMXB-A; DMBX-anabaseine) Cat. No.: HY-14564A Cat. No.: HY-B0569

Bioactivity: GTS-21 dihydrochloride is a selective α7 nicotinic Bioactivity: Hexamethonium Bromide is a non-depolarising ganglionic acetylcholine receptor agonist, has recently been established blocker, a nicotinic nACh (NN) receptor antagonist. Target: as a promising treatment for inflammation. nAChR Hexamethonium Bromide is a non-depolarising , a nicotinic nACh receptor antagonist that acts in autonomic ganglia by binding mostly in or on the NN receptor,… Purity: 99.76% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g, 5 g

Lobeline hydrochloride hydrochloride (α- hydrochloride; L-Lobeline hydrochloride) Cat. No.: HY-B0979 Cat. No.: HY-17555

Bioactivity: Lobeline hydrochloride, a nicotinic receptor agonist, acting Bioactivity: Meclofenoxate hydrochloride, an ester of as a potent antagonist at both α3β2 and α4β2 neuronal (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown nicotinic receptor subtypes. to improve memory, have a mentally stimulating effect, and improve general cognition.

Purity: 99.97% Purity: 98.32% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 100 mg, 500 mg 100 mg

Methyllycaconitine citrate Monepantel (MLA) Cat. No.: HY-N2332A (AAD1566) Cat. No.: HY-14774

Bioactivity: citrate is a specific antagonist of α7 Bioactivity: Monepantel is organic anthelmintic, and acts as a positive neuronal nicotinic acetylcholine receptor ( α7nAChR). allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor ( nAChR) subunits.

Purity: 98.0% Purity: 99.43% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

N-Methylcytisine Nelonicline (Caulophylline) Cat. No.: HY-N0443 (ABT-126) Cat. No.: HY-16748

Bioactivity: N-Methylcytisine (Caulophylline), a tricyclic quinolizidine Bioactivity: Nelonicline (ABT-126) is a selective neuronal nicotinic receptor alkaloid, exerts hypoglycaemic, and agonist. anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central

nervous system and has a high affinity ( Kd = 50 nM) to… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 250 mg, 500 mg

NS 1738 Pancuronium dibromide (NSC 213859) Cat. No.: HY-12151 Cat. No.: HY-B0429

Bioactivity: NS 1738 (NSC 213859) is a novel positive allosteric modulator Bioactivity: Pancuronium Dibromide is a bis-quaternary steroid that is a of the α7 nAChR, with respect to positive modulation of α7 competitive . Target: nAChR Pancuronium

nAChR (EC 50=3.4 μM in oocyte experiments). dibromide is a competitive AChR antagonist (IC50 = 5.5 nM) and acts as a relaxant. Pancuronium dibromide interrupts neuromuscular transmission by competing with… Purity: 99.21% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

PNU-120596 PNU-282987 (NSC 216666) Cat. No.: HY-12152 Cat. No.: HY-12560A

Bioactivity: PNU-120596 (NSC 216666 ) is a potent and selective positive Bioactivity: PNU-282987 is a selective α7 nicotinic acetylcholine allosteric α7 nAChR modulator with an EC50 of 0.2 μM. receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). IC50 value: 26 nM(Ki) [1] Target: α7 nAChR agonist in vitro: Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in… Purity: 98.15% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

PNU-282987 S enantiomer free base Cat. No.: HY-12560D (RJR-2403; (E)-Metanicotine) Cat. No.: HY-13225A

Bioactivity: PNU-282987 S enantiomer free base is the S-enantiomer of Bioactivity: Rivanicline (RJR-2403) is a neuronal nicotinic receptor PNU-282987 free base. PNU-282987 is an α7 nicotinic agonist, showing high selectivity for the α4β2 subtype (Ki=26 acetylcholine receptor (α7 nAChR) agonist. nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM). IC50 value: 26 nM [1] Target: α4β2 nAChR in vitro: At concentrations up to 1 mM, Rivanicline does not significantly… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 2 mg, 5 mg

Rivanicline hemioxalate Rivanicline oxalate (RJR-2403 (hemioxalate); (E)-Metanicotine (hemioxalate)) Cat. No.: HY-13225B (RJR-2403 (oxalate); (E)-Metanicotine (oxalate)) Cat. No.: HY-13225

Bioactivity: Rivanicline hemioxalate (RJR-2403 hemioxalate) is a neuronal Bioactivity: Rivanicline oxalate (RJR-2403 oxalate) is a neuronal nicotinic nicotinic receptor agonist, showing high selectivity for the receptor agonist, showing high selectivity for the α4β2 α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM). IC50 value: 26 nM [1] Target: α4β2 receptors(Ki= 36000 nM). nAChR in vitro: At concentrations up to 1 mM, Rivanicline does… Purity: 95.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

S16961 Sofiniclin (S169611) Cat. No.: HY-U00281 (ABT 894) Cat. No.: HY-14824

Bioactivity: S16961 is a nicotinic receptor agonist. Bioactivity: Sofiniclin (ABT 894) is an agonist of nicotinic acetylcholine receptor (nAChR), used as a potential non- treatment for attention-deficit/hyperactivity disorder (ADHD).

Purity: >98% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Tebanicline hydrochloride (Ebanicline hydrochloride; ABT-594 hydrochloride) Cat. No.: HY-14316A (CP 526555) Cat. No.: HY-10019

Bioactivity: hydrochloride (ABT594 hydrochloride) is a nAChR Bioactivity: Varenicline (CP 526555) is a selective α4β2 nicotinic with potent, orally effective analgesic activity. It (nAChR) partial agonist. inhibits the binding of cytisine to α4β2 neuronal nAChRs with

a Ki of 37 pM.

Purity: 98.00% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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Varenicline Hydrochloride Varenicline Tartrate (CP 526555 hydrochloride) Cat. No.: HY-10020 (CP 526555-18) Cat. No.: HY-10021

Bioactivity: Varenicline Hcl(CP 526555;Champix) is a nicotinic receptor Bioactivity: Varenicline Tartrate(CP 526555;Champix) is a nicotinic partial agonist; it stimulates nicotine receptors more weakly receptor partial agonist; it stimulates nicotine receptors than nicotine itself does. IC50 value: Target: nAChR more weakly than nicotine itself does. IC50 value: Target: Varenicline(CP 526555; Champix; Chantix) is a prescription α4β2 nAChR Varenicline(CP 526555; Champix; Chantix) is a used to treat . As a partial… prescription medication used to treat smoking addiction. As a… Purity: >98% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Vecuronium bromide Zaldaride maleate (ORG NC 45) Cat. No.: HY-B0118A (CGS-9343B; KW 5617) Cat. No.: HY-105118A

Bioactivity: is a nondepolarizing neuromuscular blocking Bioactivity: Zaldaride maleate (CGS-9343B) is a potent and selective agent of intermediate duration. inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase [1] [2] activity, with an IC50 of 3.3 nM . Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 5 mg

ZSET1446 (ST-101) Cat. No.: HY-11013

Bioactivity: ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.

Purity: 98.03% Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]