4′-[3-[3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4′-carbonitrile <SC>L</SC>-tartrate hydrate

产品名称：

392338-13-5
A-331440 L-tartrate hydrate
4′-[3-[3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4′-carbonitrile L-tartrate hydrate

产品介绍：

产品说明

包装

25 mg in glass bottle

生化/生理作用

Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H₃ receptors regulate release of histamine and other neurotransmitters, and histamine H₃receptor antagonists enhance neurotransmitter release. A-331440 [4′-[3-(3(R)-(dimethylamino)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile] is a histamine H₃ receptor antagonist which binds potently and selectively to both human and rat histamine H₃ receptors (K_i<=25 nM). Mice were stabilized on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H₃receptor antagonist, A-331440, has potential as an antiobesity agent.

特点和优势

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

法律信息

Subject to U.S. Patent numbers 6,515,013 and 6,620,839. Sold under license from Abbott Laboratories

基本信息

经验(实验)分子式	C₂₂H₂₇N₃O · xC₄H₆O₆ · yH₂O
分子量	349.47 (anhydrous free base basis)
PubChem化学物质编号	329770814
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	solid
颜色	white to off-white
溶解性	DMSO: ≥10 mg/mL H₂O: insoluble ethanol: insoluble methanol: insoluble
创始人	Abbott
SMILES string	[H]O[H].O[C@H]([C@@H](O)C(O)=O)C(O)=O.CN(C)[C@@H]1CCN(CCCOc2ccc(cc2)-c3ccc(cc3)C#N)C1
InChI	1S/C22H27N3O.C4H6O6.H2O/c1-24(2)21-12-14-25(17-21)13-3-15-26-22-10-8-20(9-11-22)19-6-4-18(16-23)5-7-19;5-1(3(7)8)2(6)4(9)10;/h4-11,21H,3,12-15,17H2,1-2H3;1-2,5-6H,(H,7,8)(H,9,10);1H2/t21-;1-,2-;/m11./s1
InChI key	BWZMVOINNVPOGW-LZXZYUBDSA-N

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	Eyeshields, Gloves, type N95 (US)