| 摘要 |
<p>(A) 8R- or 8S-peptide ergot alkaloids (I) having a 2-methyl substit., and their acid addition salts, are new. Pref. they also have 9,10-unsaturation and esp. are of formula (Ia):R1 is 1-4C alkyl. R2 is 1-6C alkyl or benzyl. R3 and R4 are each H or 1-4C alkyl. R5 is H or can also be bromo if R7 is H. R6 and R7 are together a bond, or both H, or R6 is methoxy and R7 is H. Also new are similar cpds. (IV) having 2-methyl replaced by R8. (R8 is CHR10-SR9. R9 is lower alkyl or benzyl. R10 is H or SR11. R11 is lower alkyl or benzyl, or together with R9 completes (CH2)n (n is 2 or 3), CH2-S-CH2 or 1,2-phenylene). (I) stimulate the dopaminergic receptors and inhibit prolactin secretion so are useful for treating Parkinsonism and acromegalia. They also enhance vigilance (e.g. treating cerebral sclerosis or traumatic loss of consciousness), are antidepressives, and have central or peripheral circulatory activity (e.g. treating migraine, orthostatic complications and prophylaxis of thrombosis). The usual oral dose is 0.5-100 mg per day.</p> |
