Lisuride, terguride and derivatives of same for use in the prevention and/or treatment of fibrotic changes

摘要

Lisuride (I), terguride (II) or a 1,1-diethyl-3-(R)-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-yl-urea derivative (III) is new, where (I)-(III) is useful for treating and/or preventing of fibrotic changes of organ and other vascular structure in human or animal for arresting and/or for remodeling of fibrotic changes of organs and their vascular structure. Lisuride (I), terguride (II) or a 1,1-diethyl-3-(R)-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-yl-urea derivative of formula (III) is new, where (I)-(III) is useful for treating and/or preventing of fibrotic changes of organ and other vascular structure in human or animal for arresting and/or for remodeling of fibrotic changes of organs and their vascular structure. R 1 : alkyl or alkynyl; R 2 : C 2H 5, n-propyl, isopropyl or alkyl; R 3 : H, CH 3, C 2H 5, isopropyl or CH 2OH; and dotted line : single or double bond. [Image] ACTIVITY : Hypotensive; Respiratory-Gen.; Cardiant; Anti-HIV; Fungicide; Antibacterial; Antiparasitic; Antiinflammatory. MECHANISM OF ACTION : 5-Hydroxytryptamine 2A receptor antagonist; 5-Hydroxytryptamine 2B receptor antagonist. The 5-hydroxytryptamine 2A receptor antagonistic activity of (I) was tested. The results showed that lisuride exhibited an IC 5 0value of 1 mmole/l.