Target Validation Information
Target ID T82543
Target Name Neuronal acetylcholine receptor protein, beta-2 chain
Target Type
Discontinued
Drug Potency against Target Sofinicline Drug Info EC50 = 40 nM [530093]
GCCSNPVCHLEHSNLC* Drug Info IC50 = 8 nM [527644]
N-methyl-N-(pyridin-3-ylmethyl)ethanamine Drug Info Ki = 28 nM [527965]
N,N-dimethyl(pyridin-3-yl)methanamine Drug Info Ki = 540 nM [527965]
(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 6000 nM [530946]
GCCSHPACAGNNQHIC* Drug Info IC50 = 1.1 nM [527644]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine Drug Info Ki = 113 nM [527965]
HOMOEPIBATIDINE Drug Info Ki = 0.127 nM [528394]
N,N-dimethyl-2-(pyridin-3-yloxy)ethanamine Drug Info Ki = 21 nM [527965]
N-ethyl-N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine Drug Info Ki = 1770 nM [527965]
N-methyl-2-(pyridin-3-yloxy)ethanamine Drug Info Ki = 35 nM [527965]
3-[2-(N,N,N-trimethylammonium)ethoxy]pyridine Drug Info Ki = 0.5 nM [528245]
6'-methylepibatidine Drug Info Ki = 256 nM [529145]
CYTISINE Drug Info Ki = 2.59 nM [528394]
N,N-dimethyl-4-(pyridin-3-yl)but-3-yn-1-amine Drug Info Ki = 510 nM [527965]
BOLDINE Drug Info Ki = 3000 nM [528761]
(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol Drug Info IC50 = 6400 nM [530946]
Predicentrine methiodide Drug Info Ki = 970 nM [528761]
The Effect of Target Knockout, Knockdown or Genetic Variations beta2 nAChR subunit knockout mice, alpha7 nAChR subunit knockout mice, and their wild-type littermates received either nicotine or saline 5 minutes before training and testing. Mice were trained using five conditioned stimulus (CS; 30 s, 85 dB white noise)--trace (30 s)--unconditioned stimulus (US; 2 s footshock) pairings. Freezing to the context and freezing to the CS were assessed 24 h later.Both contextual and trace cued fear conditioning were enhanced by nicotine administration in wild-type littermates and in alpha7 nAChR subunit knockout mice. In contrast, neither contextual fear conditioning nor trace cued fear conditioning was enhanced by nicotine administration in beta2 nAChR subunit knockout mice.These results suggest that beta2 subunit-containing nAChRs butnot alpha7 nAChR subunit-containing nAChRs are critically involved in the enhancing effect of nicotine on contextual and trace cued fear conditioning. [530093]
References
Ref 530093J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. Epub 2009 Apr 23.In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
Ref 527644J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 530946J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Ref 527644J Med Chem. 2005 Jul 28;48(15):4705-45.Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 528394Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 528245Bioorg Med Chem Lett. 2006 Aug 15;16(16):4283-6. Epub 2006 Jun 9.Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.
Ref 529145J Med Chem. 2007 Dec 13;50(25):6383-91. Epub 2007 Nov 10.Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine.
Ref 528394Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7. Epub 2006 Aug 28.Epibatidine isomers and analogues: structure-activity relationships.
Ref 527965Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6. Epub 2006 Jan 18.Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594.
Ref 528761Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.
Ref 530946J Med Chem. 2010 Jun 24;53(12):4731-48.Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Ref 528761Bioorg Med Chem. 2007 May 15;15(10):3368-72. Epub 2007 Mar 13.Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers.

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