Die vorliegende Erfindung beschreibt die Verwendung von 5-HT2- Rezeptor- Antagonisten und besonders von 8-α-Ergolinen wie Lisurid, Tergurid und deren Derivaten als 5-HT2B- und 5-HT2A-Rezeptor-Antagonisten und Antioxidantien in bevorzugt höher dosierter und bevorzugt kontinuierlicher Anwendung zur Therapie, Progressionsprophylaxe und generellen Prophylaxe von Organfibrosen und anderen, durch mesenchymale Proliferation verursachten pathologischem Organumbau.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.
