A-331440 dihydrochloride

C₂₂H₂₇N₃O · 2HCl

422.39

MFCD08705336

24724398

NA.77

A-331440 dihydrochloride is a non-imidazole H₃ histamine receptor antagonist. Presynaptic histamine H(3) receptors regulate 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 potently 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.

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
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.

100

≥98% (HPLC)

solid

desiccated

white to off-white

H₂O: ≥10 mg/mL

Abbott

2-8℃

CN([C@H]1CN(CCCOC2=CC=C(C3=CC=C(C#N)C=C3)C=C2)CC1)C.[H]Cl.[H]Cl

1S/C22H27N3O.2ClH/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;;/h4-11,21H,3,12-15,17H2,1-2H3;2*1H/t21-;;/m1../s1

XFPYVTSGYYMTFS-GHVWMZMZSA-N

5, 25 mg in glass bottle

11 - Combustible Solids

WGK 3

Eyeshields, Gloves, type N95 (US)