Agent for prophylaxis and treating of pancreatitis

Details Agent for prophylaxis and treating of pancreatitis Agent for prophylaxis and treating of pancreatitis

G - Physics

01

N

G01N 33/50 (2006.01) A61K 45/00 (2006.01) A61P 1/18 (2006.01) A61P 43/00 (2006.01) G01N 33/15 (2006.01) A61K 31/517 (2006.01) C07D 401/06 (2006.01) C07D 471/04 (2006.01) C07D 471/10 (2006.01)

Patent

CA 2607524

A pharmaceutical composition for preventing and treating pancreatitis comprising as an active ingredient, a 5-HT2A receptor antagonist, characterized in that the binding activity (pKi) of the 5-HT2A receptor antagonist to 5-HT2A receptor is higher by a value of not less than 1.0 than the binding activity to 5-HT2B and 5-HT2C receptors is disclosed. The binding activity (pKi) of the 5-HT2A receptor antagonist to 5-HT2A receptor is preferably 7.0 or higher and more preferably 8.0 or higher. The invention also provides a method of identifying a candidate substance of the agent for preventing/treating pancreatitis comprising measuring whether or not a test substance has a 5-HT2A receptor antagonism.

La présente invention concerne une composition pharmaceutique destinée à prévenir et à traiter la pancréatite comprenant en tant que principe actif, un antagoniste du récepteur de 5-HT2A, caractérisée en ce que l~activité de liaison (pKi) de l~antagoniste du récepteur 5-HT2A au récepteur 5-HT2A est supérieure d~une valeur d~au moins 1,0 à l~activité de liaison aux récepteurs 5-HT2B et 5-HT2C. L~activité de liaison (pKi) de l~antagoniste du récepteur 5-HT2A au récepteur 5-HT2A est de préférence 7,0 ou plus, idéalement 8,0 ou plus. L~invention concerne également un procédé d~identification d~une substance candidate pour l~agent destiné à la prévention/le traitement de la pancréatite comprenant le fait de mesurer si oui ou non une substance test présente un antagonisme du récepteur 5-HT2A.

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