FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to 3-substituted 1-arylindole of the formula (I) where Ar - phenyl possibly substituted with halogen atom; X is OCH2,CH2 or CH2CH2; dotted line means the optional bond; R1-R4 - hydrogen, halogen atom, lower alkyl, lower alkoxy-, hydroxy-, nitro-, lower alkylthio-, lower alkylsulfonyl-, lower alkyl- or dialkylamino-, cyano-, trifluoromethyl-, trifluoro- -methylsulfonylhydroxy- and trifluoromethylthio-group; R5 - hydrogen atom, hydroxy-, lower alkoxy-group, halogen atom, trifluoromethyl-, lower alkyl group optionally substituted with hydroxy-group, or lower alkenyl optionally substituted with hydroxyl; R6,R8 - hydrogen atom; R8 - lower alkyl, lower alkenyl (other values are given in p. 1 of the invention claim). These compounds show the basic antiserotoninergic activity and some of their - an additional antidopamine-ergic activity. Compounds of the formula (I) can be used for treatment of patients with anxiety, aggression, depression, sleep disorder, migraine, schizophrenia by binding 5HT2--receptors and D2--receptors. EFFECT: valuable pharmacological properties of compounds. 12 cl, 1 tbl, 16 ex
Title |
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Author |
Number |
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