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

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About This Item

Empirical Formula (Hill Notation):

C₂₈H₃₀N₄O · HCl · xH₂O

CAS Number:

215804-67-4

Molecular Weight:

475.02 (anhydrous basis)

MDL number:

MFCD16875431

UNSPSC Code:

12352200

PubChem Substance ID:

329824542

NACRES:

NA.77

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Quality Level

100

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 Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number

024M4612V

119K4622

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