S4326

SB-277011-A hydrochloride hydrate

≥98% (HPLC)

• Formule empirique (notation de Hill) : C₂₈H₃₀N₄O · HCl · xH₂O
• CAS Number: 215804-67-4
• Poids moléculaire : 475.02 (anhydrous basis)
• Numéro MDL: MFCD16875431
• Code UNSPSC : 12352200
• ID de substance PubChem : 329824542
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: powder
• Conditions de stockage: protect from light
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear (warmed)
• Auteur: GlaxoSmithKline
• Température de stockage: 2-8°C
• Chaîne SMILES: 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-;;
• Clé InChI: OOWNBQACGIKNGM-ONAIBGCWSA-N

Description

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.

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable