S4326
SB-277011-A hydrochloride hydrate
≥98% (HPLC)
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About This Item
Empirical Formula (Hill Notation):
C28H30N4O · HCl · xH2O
CAS Number:
Molecular Weight:
475.02 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
protect from light
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
originator
GlaxoSmithKline
storage temp.
2-8°C
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
Application
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.
Biochem/physiol Actions
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.
Features and Benefits
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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
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
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)
Amine Bahi et al.
Alcoholism, clinical and experimental research, 38(9), 2369-2376 (2014-09-27)
It has been reported that dopamine D3 receptor (D3R) knockout mice display similar ethanol (EtOH) consumption compared to wild types. In addition, studies with D3R pharmacological targeting were inconclusive. In the current study, we used both gain- and loss-of-function approaches
Global Trade Item Number
| SKU | GTIN |
|---|---|
| S4326-5MG | 04061832072517 |
| S4326-25MG | 04061836926014 |
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