| Identification | Back Directory | [Name]
(3R)-N-[6-(1H-Imidazol-1-yl)-4-pyrimidinyl]spiro[1-azabicyclo[2.2.2]octane-3,5'(4'H)-oxazol]-2'-amine | [CAS]
1221973-93-8 | [Synonyms]
(R)-N-(6-(1H-IMIDAZOL-1-YL)PYRIMIDIN-4-YL)-4`H-4-AZASPIRO[BICYCLO[2.2.2]OCTANE-2,5`-OXAZOL]-2`-AMINE
(3R)-N-[6-(1H-Imidazol-1-yl)-4-pyrimidinyl]spiro[1-azabicyclo[2.2.2]octane-3,5'(4'H)-oxazol]-2'-amine | [Molecular Formula]
C16H19N7O | [MDL Number]
MFCD31536985 | [MOL File]
1221973-93-8.mol | [Molecular Weight]
325.37 |
| Hazard Information | Back Directory | [Description]
BMS-933043 is a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. BMS-933043 showed potent binding affinity to native rat (Ki = 3.3 nM) and recombinant human alpha7 nicotinic acetylcholine receptors (Ki = 8.1 nM) and agonist activity in a calcium fluorescence assay (EC50 = 23.4 nM) and whole cell voltage clamp electrophysiology (EC50 = 0.14 micromolar (rat) and 0.29 micromolar (human)). BMS-933043 showed no agonist or antagonist activity at other nicotinic acetylcholine receptor subtypes and was at least 300 fold weaker at binding to and antagonizing human 5-HT3A receptors (Ki = 2,451 nM; IC50 = 8,066 nM). | [Uses]
BMS-933043 is a potent and selective α7 nACh receptor partial agonist. BMS-933043 attenuates the cognitive impairment in mice and can be utilized in research related to cognitive dysfunction in schizophrenia[1]. | [References]
[1] King D, et al. BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia. ACS Med Chem Lett. 2017 Feb 8;8(3):366-371. DOI:10.1021/acsmedchemlett.7b00032 |
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