A-331440 dihydrochloride (CAS 392338-13-5)
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A non-imidazole H3 histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate the release of histamine and other neurotransmitters, and histamine H(3) receptor antagonists enhance neurotransmitter release. A-331440 is a histamine H(3) receptor antagonist, which binds strongly and selectively to both human and rat histamine H(3) receptors (K(i)=25 nM). Mice 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. Both data shows that the histamine H(3) receptor antagonist, A-331440, has potential as an antiobesity agent.
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
A-331440 dihydrochloride, 5 mg | sc-252330 | 5 mg | $150.00 |