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A 331440 dihydrochloride Sale

目录号 : GC13537

H3 receptor antagonist,non-imidazole,high affinity

A 331440 dihydrochloride Chemical Structure

Cas No.:1049740-32-0

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10mg
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50mg
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产品描述

A-331440 is described here instead of A-331440 dihydrochloride. A-331440 is an antagonist of non-imidazole histamine H3 receptor with an IC50 value of 22.7 nM for human cortex histamine H3 [1].

Histamine, as a neurotransmitter, is important in homeostasis and physiology. In the CNS, histamine released has the potential to interact with H1, H2, H3 and possibly H4 receptors. All the receptors are G-protein coupled receptors [2].

In HEK 293 cells stably transfected with rat or human histamine H3 receptors, A-331440 was tested for its ability to antagonize increasing calcium mobilization in response to (R)-α-methylhistamine and showed pKb ± S.E.M. values of 7.38 ± 0.10 and 7.37 ± 0.29 for rat histamine H3 and human histamine H3, respectively [1].

In mice, treatment with A-331440 at a dose of 100 mg/kg resulted in piloerection and hypoactivity in the first 2 h, but diminished thereafter. In naive male CD-1 mice, administration with comparable doses of A-331440 i.p. also produced similar data. By day 28, mice treated with A-331440 at the intermediate dose weighed 35.7 ± 0.93 g with an average weight loss of 5.3 ± 0.99 g. The high dose of A-331440 (15 mg/kg, p.o., b.i.d.) produced a marked and sustained weight loss [1].

References:
[1].  Hancock AA, Bennani YL, Bush EN, et al. Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. European journal of pharmacology, 2004, 487(1): 183-197.
[2].  Hancock AA, Diehl MS, Faghih R, et al. In vitro Optimization of Structure Activity Relationships of Analogues of A-331440 Combining Radioligand Receptor Binding Assays and Micronucleus Assays of Potential Antiobesity Histamine H3 Receptor Antagonists. Basic & clinical pharmacology & toxicology, 2004, 95(3): 144-152.

Chemical Properties

Cas No. 1049740-32-0 SDF
化学名 (R)-4'-(3-(3-(dimethylamino)pyrrolidin-1-yl)propoxy)-[1,1'-biphenyl]-4-carbonitrile dihydrochloride
Canonical SMILES CN([C@](C1)([H])CCN1CCCOC2=CC=C(C3=CC=C(C#N)C=C3)C=C2)C.Cl.Cl
分子式 C22H27N3O.2HCl 分子量 422.39
溶解度 <42.24mg/ml in Water; <8.45mg/ml in DMSO 储存条件 Desiccate at RT
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1 mM 2.3675 mL 11.8374 mL 23.6748 mL
5 mM 0.4735 mL 2.3675 mL 4.735 mL
10 mM 0.2367 mL 1.1837 mL 2.3675 mL
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