Indolo[2,1-c][1,4]benzodiazepines: a new class of antiallergic agents.
A series of 12-(cyclic alkylamino)-6H-indolo[2,1-c][1,4]benzodiazepines were synthesized that possess antihistamine and antiserotonin activities as well as ability to inhibit mediator release. Compound 6a, 12-(4-methyl-1-piperazinyl)-6H-indolo[2,1-c][1,4]benzodiazepine was a more potent inhibitor of serotonin release than disodium cromoglycate (DSCG) and ketotifen and approximately equivalent to oxatomide. In the in vivo tests (PCA and ALA), compound 6a was equivalent or superior to DSCG and oxatomide. These agents have potential for the treatment of a variety of allergic conditions.
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D000707:Anaphylaxis / Q000517:prevention & control; D000818:Animals; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D004205:Cromolyn Sodium / Q000494:pharmacology; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D006967:Hypersensitivity / Q000188:drug therapy*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D012701:Serotonin / Q000378:metabolism
D006634:Histamine H1 Antagonists; D007211:Indoles; D001569:Benzodiazepines; D012701:Serotonin; D004205:Cromolyn Sodium