Name: SB-277011-A hydrochloride hydrate
Brand: SIGMA

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About This Item

经验公式（希尔记法）:

C₂₈H₃₀N₄O · HCl · xH₂O

CAS Number:

215804-67-4

分子量:

475.02 (anhydrous basis)

MDL编号:

MFCD16875431

UNSPSC代码:

12352200

PubChem化学物质编号:

329824542

NACRES:

NA.77

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质量水平

100

方案

≥98% (HPLC)

表单

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°C

SMILES字符串

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

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.

生化/生理作用

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.

SB-277011-A is the most selective D3 dopamine receptor antagonist.

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.

特点和优势

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.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.