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Inverse agonists of the histamine h3-receptor as drugs

The objective is to design and develop a histamine h3
receptor inverse agonist as a novel type of drug for use in
the treatment of alzheimer's disease, obesity and/or
epilepsy.

The main objective is to design and develop an inverse agonist of the histamine H3 receptor, a novel type of psychotropic drug in order to improve vigilance, attention and memory and regulate vestibular reflexes. These properties derive from a facilitation of histaminergic transmission in the brain and should be useful in the treatment of elderly patients affected by Alzheimer's and related diseases. In addition, since such non-amphetaminic agents decrease food intake and experimental convulsions they should be useful in the treatment of obesity and/or epilepsies. The project comprises first the selection of a full inverse agonist at the constitutively active human receptor, a compound with suitable physicochemical properties, bioavailability and lack of chronic toxicity in animals. The selected compound will then be submitted to the various pharmaceutical operations including clinical trials leading to its development as a drug useful in at least one of the above mentioned indications. All these operations will be conducted in collaboration between two European pharmaceutical companies, viz BIOPROJET (FRANCE and GRUPO FERRER (SPAIN) and dispatched according their best respective expertises. Keywords: psychotropic drug, obesity, histamine.
Acronym: 
ANTHAMINE
Project ID: 
2 582
Start date: 
27-02-2001
Project Duration: 
94months
Project costs: 
9 330 000.00€
Technological Area: 
Pharmaceutical Products / Drugs
Market Area: 

Raising the productivity and competitiveness of European businesses through technology. Boosting national economies on the international market, and strengthening the basis for sustainable prosperity and employment.