INHIBITOR AGAINST OPIOID HYDROLYZING ENZYME

NEW MATERIAL:An organogermanium compound expressed by formula I [R1 is lower alkyl; R2-R4 are H, lower alkyl or (substituted) phenyl; Z is carboxyl, benzylaminomethyl or hydrochloride thereof]. EXAMPLE:(n-C3H7)GeCH2CH2COOH. USE:An inhibitor against opioid hydrolyzing enzymes and analgesi capable of...

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Hauptverfasser: YOSHIHARA TORU, KAKIMOTO NORIHIRO, HASATO TADAHIKO
Format: Patent
Sprache:eng
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Zusammenfassung:NEW MATERIAL:An organogermanium compound expressed by formula I [R1 is lower alkyl; R2-R4 are H, lower alkyl or (substituted) phenyl; Z is carboxyl, benzylaminomethyl or hydrochloride thereof]. EXAMPLE:(n-C3H7)GeCH2CH2COOH. USE:An inhibitor against opioid hydrolyzing enzymes and analgesi capable of selectively inhibiting enzymes hydrolyzing enkephalin which is one kind of endogenous morphinic substance, e.g. aminopeptidase derived from simian brains, etc., in a low concentration. PREPARATION:For example, trichlorogermylpropionic acid expressed by formula III is reacted with a Grignard reagent expressed by the formula R1MgX in a solvent e.g. ethyl ether, etc., while heating and refluxing according to the reaction formula and the resultant product is then hydrolyzed with hydrochloric acid.