Vasodilating and hypotensive alkaloid stepharin salts - with organic acids, e.g. stepharin tosylate

摘要

New stepharin salts are of formula (I) in which A circled negative is the anion of an organic acid, A circled negative is pref. the anion of an aliphatic, araliphatic or cycloalphatic mono- di- or tricarboxylic acid or sulphonic acid which can be so substd. by OR1 or NR1R2 gps. (where R1 and R2 are H, 1-4C alkyl or acyl with 1-4C alkyl that at least one acidic gp. is present in excess or of an aromatic or heterocyclic mono- di or tricarboxylic or sulphonic which can be so substd. by 1-4C alkyl, OH, 1-4C alkoxy, amino, 1-4C mono-, or dialkyl-amino, 1-4C acylamino, NO2 or halogen that at least one acidic gp. is present in excess. The new salts of the known alkaloid stepharin have strong vasodilating and blood press. lowering properties. (I) can be used for treatment of cardiac, cardiovascular and circulatory disorders, e.g. essential and malignant hypertension, cardiac muscle hyper function, angina pectoris, and peripheral vascular disorders such as Raynaud's disease and thromboangitis obliterans. The desirable effects of (I) are unaccompanied by alpha-blocking, beta-blocking, sedative, depressant, adrenergic neurone blocking or ganglionic blocking effects. The toxicity of (I) is very low. Specific salts (I) include stepharin p-toluenesulphonate.