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
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关于此项目
经验公式（希尔记法）:
C22H27N3O · xC4H6O6 · yH2O
化学文摘社编号:
分子量:
349.47 (anhydrous free base basis)
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
assay
≥98% (HPLC)
form
solid
color
white to off-white
solubility
DMSO: ≥10 mg/mL, H2O: insoluble, ethanol: insoluble, methanol: insoluble
originator
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
Biochem/physiol Actions
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 (Ki<=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.
Features and Benefits
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.
Legal Information
Subject to U.S. Patent numbers 6,515,013 and 6,620,839. Sold under license from Abbott Laboratories
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)