SB-277011-A hydrochloride hydrate

产品说明

应用

SB-277011-A hydrochloride hydrate has been used:

• as a dopamine D3 receptor-selective antagonist in rats to test its effect on 4-propyl-9-hydroxynaphthoxazine ([3H]-(+)-PHNO) radiotracer in cerebellum L9/10 and striatum
• as an acetylcholine inhibitor to test its negative allosteric modulation on Ascaris suum nicotinic acetylcholine receptor (Asu-ACR-16) expressed in Xenopus oocytes and its inhibitory effect on locomotion in Caenorhabditis elegans
• to test its effect on alcohol consumption in mice

SB-277011-A hydrochloride hydrate may be used in D3 dopamine receptor-mediated cell signaling studies.

包装

5, 25 mg in glass bottle

生化/生理作用

The D₃ dopamine receptor antagonist, SB-277011-A inhibits the cocaine-seeking behavior and cocaine-enhances brain stimulation reward in in rats. It decreases drug-seeking behavior and may be useful in treatment of cocaine and methamphetamine addiction.
SB-277011-A is a potent, selective brain-penetrant D3 dopamine receptor antagonist; 80-100x selective for D3 over D2; pKi = 7.95 for hD3 receptor.

特点和优势

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

基本信息

经验(实验)分子式	C28H30N4O · HCl · xH2O
分子量	475.02 (anhydrous basis)
MDL编号	MFCD16875431
PubChem化学物质编号	329824542

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
储存条件	protect from light
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear (warmed)
创始人	GlaxoSmithKline
储存温度	2-8℃
SMILES string	O.Cl.O=C(N[C@@H]1CC[C@H](CC1)CCN2CCc3cc(ccc3C2)C#N)c4ccnc5ccccc45
InChI	1S/C28H30N4O.ClH.H2O/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27;;/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33);1H;1H2/t20-,24-;;
InChI key	OOWNBQACGIKNGM-ONAIBGCWSA-N

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable