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A7730 Sigma

A-331440 dihydrochloride

≥98% (HPLC), solid

Synonym: 4’-[3-[(3(R)-Dimethylamino-1-pyrrolidinyl]propoxy]-[1,1-biphenyl]-4‘-carbonitrile dihydrochloride




5, 25 mg in glass bottle

Biochem/physiol Actions

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.

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.

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Safety Information

GHS07  GHS07
Signal word 
Hazard statements 
Precautionary statements 
NONH for all modes of transport
WGK Germany 


Certificate of Analysis

Protocols & Articles


Histamine Receptors

The biogenic amine histamine plays an important role in a variety of pathophysiological conditions. In peripheral tissues, histamine is mainly stored in mast cells and basophils. In allergic conditio...
Keywords: Alzheimer Disease, Atomic absorption spectroscopy, Cardiovascular, Clinical, Diseases, Gene expression, Inflammation, Ligands, Neurotransmitters, Obesity, Transduction

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