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nAChR Nicotinic acetylcholine receptors nAChRs (nicotinic acetylcholine receptors) are neuron receptor proteins that signal for muscular contraction upon a chemical stimulus. They are cholinergic receptors that form ligand-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 acetylcholine receptor-the muscarinic acetylcholine receptor (mAChR)-the nAChR is triggered by the binding of the neurotransmitter acetylcholine (ACh). Just as muscarinic receptors are named such because they are also activated by muscarine, nicotinic receptors can be opened not only by acetylcholine but also by nicotine —hence the name "nicotinic". www.MedChemExpress.com 1 nAChR Agonists, Antagonists, Inhibitors, Activators & Modulators (+)-Sparteine (-)-(S)-B-973B Cat. No.: HY-W008350 Cat. No.: HY-114269 (+)-Sparteine is a natural alkaloid acting as a (-)-(S)-B-973B is a potent allosteric agonist and ganglionic blocking agent. (+)-Sparteine positive allosteric modulator of α7 nAChR, with competitively blocks nicotinic ACh receptor in the antinociceptive activity. neurons. Purity: ≥97.0% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg (R)-(+)-Anatabine (Rac)-ABT-202 dihydrochloride Cat. No.: HY-126047B Cat. No.: HY-124540B (R)-(+)-Anatabine is an less active R-enantiomer (Rac)-ABT-202 dihydrochloride is a racemate of of Anatabine. Anatabine is a potent α4β2 nAChR ABT-202. ABT-202 is an agonist of nicotinic agonist. Anatabine inhibits NF-κB activation acetylcholine receptors (nAChRs) and can be used lower amyloid-β (Aβ) production by preventing as an analgesic. the β-cleavage of amyloid precursor protein (APP). Purity: >98% Purity: ≥95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg (rel)-Asperparaline A (S)-UFR2709 ((rel)-Aspergillimide; (rel)-VM55598) Cat. No.: HY-124874 Cat. No.: HY-137231A (rel)-Asperparaline A ((rel)-Aspergillimide), an (S)-UFR2709 is a competitive nAChR anthelmintic metabolite, is isolated from okara antagonist and displays higher affinity for that has been fermented with Aspergillus japonicas α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 JV-23. (rel)-Asperparaline A is also a potent and decreases anxiety and reduces ethanol consumption selective antagonist of nAChR. and ethanol preference in alcohol-preferring rats. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg (S)-UFR2709 hydrochloride (±)-Anatoxin A fumarate Cat. No.: HY-137231B Cat. No.: HY-N2326 (S)-UFR2709 (hydrochloride) is a competitive (±)-Anatoxin A fumarate is a natural alkaloid nAChR antagonist and displays higher isolated from freshwater affinity for α4β2 nAChRs than for α7 nAChRs. cyanobacterium. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. Purity: 98.08% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg 3-Bromocytisine 5-AAM-2-CP (3-Br-cytisine) Cat. No.: HY-107684 Cat. No.: HY-136608 3-Bromocytisine (3-Br-cytisine) is a potent nACh 5-AAM-2-CP is a major metabolite of Acetamiprid. receptors agonist, with IC50s are 0.28, 0.30 and Acetamiprid is a neonicotinoid insecticide used 31.6 nM for hα4β4, hα4β2, and hα7-nACh, worldwide and is a nAChR agonist. respectively. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] 5-AMAM-2-CP A-582941 dihydrochloride Cat. No.: HY-136609 Cat. No.: HY-59201A 5-AMAM-2-CP is a major metabolite of Acetamiprid. A-582941 dihydrochloride is a potent, selective Acetamiprid is a neonicotinoid insecticide used and brain-penetrant partial agonist of α7 nAChR, worldwide and is a nAChR agonist. with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 25 mg Size: 1 mg, 5 mg A-867744 ABT-107 Cat. No.: HY-12149 Cat. No.: HY-108038 A-867744 is a highly potent and selective type II ABT-107 is a selective α7 neuronal nicotinic positive allosteric modulator (PAM) of the alpha7 receptor agonist. ABT-107 protects against nicotinic acetylcholine receptors (nAChR) with an nigrostriatal damage in rats with unilateral EC50 of 1.0 μM. 6-hydroxydopamine lesions. Purity: 99.92% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg ABT-418 hydrochloride Acetamiprid Cat. No.: HY-105170B Cat. No.: HY-B0823 ABT-418 hydrochloride is a potent and selective Acetamiprid is a neonicotinoid insecticide used agonist of nAChRs with cognitive enhancing and worldwide. Acetamiprid is a nicotinic acetylcholine anxiolytic activities. ABT-418 hydrochloride receptor (nAChR) agonist, and is shown to be activates cholinergic channel and can be used for associated with neuromuscular and reproductive research of Alzheimer's disease. disorders. Purity: 99.53% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 100 mg Acetylcholine chloride Adiphenine hydrochloride (ACh chloride) Cat. No.: HY-B0282 Cat. No.: HY-B0379A Acetylcholine chloride (ACh chloride), a Adiphenine hydrochloride is a non-competitive neurotransmitter, is a potent cholinergic agonist. inhibitor of nicotinic acetylcholine receptor Acetylcholine chloride is a modulator of the (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 activity of dopaminergic (DAergic) neurons through µM for α1, α3β4, α4β2, and α4β4, respectively. the stimulation of nicotinic acetylcholine Adiphenine hydrochloride has narcotic and receptors (nAChRs). anticonvulsant effects. Purity: ≥98.0% Purity: 99.77% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 10 mM × 1 mL, 100 mg Anabasine Anabasine hydrochloride ((S)-Anabasine; (+)-Anabasine) Cat. No.: HY-B1532 ((S)-Anabasine hydrochloride; (+)-Anabasine hydrochloride)Cat. No.: HY-W014928 Anabasine ((S)-Anabasine) is an alkaloid that Anabasine ((S)-Anabasine) hydrochloride is an found as a minor component in tobacco (Nicotiana). alkaloid that found as a minor component in tobacco Anabasine is a (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors full agonist of nicotinic acetylcholine receptors (nAChRs). (nAChRs). Purity: 98.57% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg www.MedChemExpress.com 3 Anatabine dicitrate Aniracetam Cat. No.: HY-19918A (Ro 13-5057) Cat. No.: HY-10932 Anatabine dicitrate is a tobacco alkaloid that can Aniracetam(Ro 13-5057) is a nootropics and cross the blood-brain barrier. Anatabine dicitrate neuroprotective drug, which is selectively is a potent α4β2 nAChR agonist. modulates the AMPA receptor and nAChR. Target: AMPA; nAChR Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam. Purity: 99.24% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g AR-R17779 hydrochloride Asoxime dichloride Cat. No.: HY-135483A (HI-6) Cat. No.: HY-106901A AR-R17779 hydrochloride is a potent and selective Asoxime dichloride (HI-6) is an antagonist to full agonist of nAChR, with Kis of 92 and 16000 acetylcholine receptors (AChRs) including the nM for α7 and α4β2 subtype, respectively. nicotinic receptor, α7 nAChR. Asoxime dichloride AR-R17779 hydrochloride can improve learning and involves in modulating immunity response. memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Atracurium besylate Benzethonium chloride (BW-33A) Cat. No.: HY-B0292A Cat. No.: HY-B0942 Atracurium Besylate is a neuromuscular blocking Benzethonium chloride inhibit human recombinant α7 agent with ED95 of 0.2 mg/kg. and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes. Purity: 98.89% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg Benzoquinonium dibromide BNC210 Cat. No.: HY-B1552B (H-Ile-Trp-OH; IW-2143) Cat. No.: HY-105858 Benzoquinonium dibromide is a nicotinic BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR acetylcholine receptors (nAChRs) antagonist, with negative allosteric modulator. BNC210 has potent an IC50 of 0.46 μM. Benzoquinonium dibromide can activity in animal models of anxiety and block neuromuscular and ganglionic transmission. depression. Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg BNC375 Catestatin Cat. No.: HY-128575 Cat. No.: HY-P1271 BNC375 is a potent, selective, and orally Catestatin is a 21-amino acid residue, cationic available type I positive allosteric modulator of and hydrophobic peptide. Catestatin is an α7 nAChRs with an EC50 of 1.9 μM.
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  • (19) United States (12) Patent Application Publication (10) Pub

    (19) United States (12) Patent Application Publication (10) Pub

    US 20130289061A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2013/0289061 A1 Bhide et al. (43) Pub. Date: Oct. 31, 2013 (54) METHODS AND COMPOSITIONS TO Publication Classi?cation PREVENT ADDICTION (51) Int. Cl. (71) Applicant: The General Hospital Corporation, A61K 31/485 (2006-01) Boston’ MA (Us) A61K 31/4458 (2006.01) (52) U.S. Cl. (72) Inventors: Pradeep G. Bhide; Peabody, MA (US); CPC """"" " A61K31/485 (201301); ‘4161223011? Jmm‘“ Zhu’ Ansm’ MA. (Us); USPC ......... .. 514/282; 514/317; 514/654; 514/618; Thomas J. Spencer; Carhsle; MA (US); 514/279 Joseph Biederman; Brookline; MA (Us) (57) ABSTRACT Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject (21) App1_ NO_; 13/924,815 comprising; administering a therapeutic amount of the neu rological stimulant and administering an antagonist of the kappa opioid receptor; to thereby reduce or prevent the devel - . opment of aversion to the CNS stimulant in the subject. Also (22) Flled' Jun‘ 24’ 2013 disclosed is a method of reducing or preventing the develop ment of addiction to a CNS stimulant in a subj ect; comprising; _ _ administering the CNS stimulant and administering a mu Related U‘s‘ Apphcatlon Data opioid receptor antagonist to thereby reduce or prevent the (63) Continuation of application NO 13/389,959, ?led on development of addiction to the CNS stimulant in the subject. Apt 27’ 2012’ ?led as application NO_ PCT/US2010/ Also disclosed are pharmaceutical compositions comprising 045486 on Aug' 13 2010' a central nervous system stimulant and an opioid receptor ’ antagonist.