A3104

A-331440 L-tartrate hydrate

≥98% (HPLC), solid

• Sinônimo(s): 4′-[3-[3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4′-carbonitrile L-tartrate hydrate
• Fórmula empírica (Notação de Hill): C₂₂H₂₇N₃O · xC₄H₆O₆ · yH₂O
• Número CAS: 392338-13-5
• Peso molecular: 349.47 (anhydrous free base basis)
• Código UNSPSC: 12352202
• ID de substância PubChem: 329770814
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Formulário: solid
• cor: white to off-white
• solubilidade: DMSO: ≥10 mg/mL; H₂O: insoluble; ethanol: insoluble; methanol: insoluble
• originador: Abbott
• cadeia de caracteres SMILES: [H]O[H].O[C@H]([C@@H](O)C(O)=O)C(O)=O.CN(C)[C@@H]1CCN(CCCOc2ccc(cc2)-c3ccc(cc3)C#N)C1
• InChI: 1S/C22H27N3O.C4H6O6.H2O/c1-24(2)21-12-14-25(17-21)13-3-15-26-22-10-8-20(9-11-22)19-6-4-18(16-23)5-7-19;5-1(3(7)8)2(6)4(9)10;/h4-11,21H,3,12-15,17H2,1-2H3;1-2,5-6H,(H,7,8)(H,9,10);1H2/t21-;1-,2-;/m11./s1
• chave InChI: BWZMVOINNVPOGW-LZXZYUBDSA-N

Descrição

Ações bioquímicas/fisiológicas

A-331430 L-tartrate hydrate is a non-imidazole H₃ histamine receptor antagonist.

Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H₃ receptors regulate release of histamine and other neurotransmitters, and histamine H₃ receptor antagonists enhance neurotransmitter release. A-331440 [4′-[3-(3(R)-(dimethylamino)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile] is a histamine H₃ receptor antagonist which binds potently and selectively to both human and rat histamine H₃ receptors (K_i<=25 nM). Mice were stabilized on a high-fat diet (45 kcal % lard) prior to 28-day oral b.i.d. dosing for measurement of obesity-related parameters. A-331440 administered at 0.5 mg/kg had no significant effect on weight, whereas 5 mg/kg decreased weight comparably to dexfenfluramine (10 mg/kg). A-331440 administered at 15 mg/kg reduced weight to a level comparable to mice on the low-fat diet. The two higher doses reduced body fat and the highest dose also normalized an insulin tolerance test. These data show that the histamine H₃ receptor antagonist, A-331440, has potential as an antiobesity agent.

Características e benefícios

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Informações legais

Subject to U.S. Patent numbers 6,515,013 and 6,620,839. Sold under license from Abbott Laboratories

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable
• Equipamento de proteção individual: Eyeshields, Gloves, type N95 (US)