A3104

A-331440 L-tartrate hydrate

≥98% (HPLC), solid

• 别名: 4′-[3-[3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4′-carbonitrile L-tartrate hydrate
• 经验公式（希尔记法）: C₂₂H₂₇N₃O · xC₄H₆O₆ · yH₂O
• CAS号: 392338-13-5
• 分子量: 349.47 (anhydrous free base basis)
• 分類程式碼代碼: 12352202
• PubChem物質ID: 329770814
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 顏色: white to off-white
• 溶解度: DMSO: ≥10 mg/mL; H₂O: insoluble; ethanol: insoluble; methanol: insoluble
• 起源: Abbott
• SMILES 字串: [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 密鑰: BWZMVOINNVPOGW-LZXZYUBDSA-N

说明

生化／生理作用

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.

特點和優勢

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.

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable
• 個人防護裝備: Eyeshields, Gloves, type N95 (US)