S4326

SB-277011-A hydrochloride hydrate

≥98% (HPLC)

• Empirische Formel (Hill-System): C₂₈H₃₀N₄O · HCl · xH₂O
• CAS-Nummer: 215804-67-4
• Molekulargewicht: 475.02 (anhydrous basis)
• NACRES: NA.77
• PubChem Substance ID: 329824542
• UNSPSC Code: 12352200
• MDL number: MFCD16875431
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: protect from light

Eigenschaften

• Quality Segment: 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

Beschreibung

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

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.

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

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.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable