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About This Item
經驗公式（希爾表示法）:
C28H30N4O · HCl · xH2O
CAS號碼:
分子量：:
475.02 (anhydrous basis)
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
推薦產品
品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
protect from light
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear (warmed)
起源
GlaxoSmithKline
儲存溫度
2-8°C
SMILES 字串
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 密鑰
OOWNBQACGIKNGM-ONAIBGCWSA-N
應用
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.
特點和優勢
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Jeremy G Gilbert et al.
Synapse (New York, N.Y.), 57(1), 17-28 (2005-04-29)
Recent studies have shown that the novel dopamine (DA) D3 receptor antagonists SB-277011A and NGB 2904 inhibit cocaine- and/or stress-induced reinstatement of drug-seeking behavior. The present study sought to determine if SB-277011A, NGB 2904, or BP-897 (a mixed D3 agonist/antagonist)
Krista Spiller et al.
Psychopharmacology, 196(4), 533-542 (2007-11-07)
We have previously reported that selective antagonism of brain D3 receptors by SB-277011A or NGB 2904 significantly attenuates cocaine- or nicotine-enhanced brain stimulation reward (BSR). In the present study, we investigated whether the selective D3 receptor antagonists SB-277011A and NGB
Zheng-Xiong Xi et al.
The European journal of neuroscience, 21(12), 3427-3438 (2005-07-20)
In rats, acute administration of SB-277011A, a highly selective dopamine (DA) D(3) receptor antagonist, blocks cocaine-enhanced brain stimulation reward, cocaine-seeking behaviour and reinstatement of cocaine-seeking behaviour. Here, we investigated whether SB-277011A attenuates cocaine reinforcement as assessed by cocaine self-administration under
Fudan Zheng et al.
International journal for parasitology. Drugs and drug resistance, 6(1), 60-73 (2016-04-08)
Soil-transmitted helminth infections in humans and livestock cause significant debility, reduced productivity and economic losses globally. There are a limited number of effective anthelmintic drugs available for treating helminths infections, and their frequent use has led to the development of
Satoko Baba et al.
Journal of pharmacological sciences, 127(3), 326-331 (2015-04-04)
Antagonism of the dopamine D3 receptor has been hypothesized to be beneficial for schizophrenia cognitive deficits, negative symptoms and extrapyramidal symptoms. However, recent animal and human studies have shown that most antipsychotics do not occupy D3 receptors in vivo, despite their
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