A3104

A-331440 L-tartrate hydrate

≥98% (HPLC), solid

• 동의어(들): 4′-[3-[3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4′-carbonitrile L-tartrate hydrate
• 실험식(Hill 표기법): C₂₂H₂₇N₃O · xC₄H₆O₆ · yH₂O
• CAS Number: 392338-13-5
• Molecular Weight: 349.47 (anhydrous free base basis)
• UNSPSC 코드: 12352202
• PubChem Substance ID: 329770814
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 양식: solid
• 색상: white to off-white
• solubility: DMSO: ≥10 mg/mL; H₂O: insoluble; ethanol: insoluble; methanol: insoluble
• 주관자: Abbott
• SMILES string: [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
• InChI key: BWZMVOINNVPOGW-LZXZYUBDSA-N

설명

생화학적/생리학적 작용

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.

특징 및 장점

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable
• 개인 보호 장비: Eyeshields, Gloves, type N95 (US)