title: In vitro effects of the antiallergy compound, CI-949, on interleukin-1 and 2 release, and on mitogen and alloantigen responsiveness.
abstract: CI-949 (5-methoxy-3-(1-methylethoxy)-1-phenyl-N-1H-tetrazol-5-yl-1H -indole- 2-carboxamide, L-arginine salt), an antiallergy compound, was found to be a weak inhibitor of IL-1 release from LPS-stimulated murine peritoneal exudate cells and human peripheral blood leukocytes, with IC50S of 186.2 and 267.9 microM, respectively. CI-949 was also a poor inhibitor of release of IL-2 from Con A-stimulated rat splenocytes (37% inhibition at 100 microM). CI-949 did produce concentration-related inhibition of the response of human lymphocytes to PHA and Con A (IC50S = 44.7 and 21.5 microM, respectively) as well as in the mixed lymphocyte reaction (MLR) (IC50 = 16.8 microM). The clinical significance of these latter findings is unknown at present.
authors.affiliation: Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105.
authors.forename: R B
authors.initials: RB
authors.lastname: Gilbertsen
authors.forename: K M
authors.initials: KM
authors.lastname: Cullinen
authors.forename: D J
authors.initials: DJ
authors.lastname: Wilburn
authors.forename: M K
authors.initials: MK
authors.lastname: Dong
authors.forename: M C
authors.initials: MC
authors.lastname: Conroy
mesh_terms: D000818:Animals; D001169:Arthritis, Experimental / Q000378:metabolism; D001393:Azoles / Q000494:pharmacology*; D006801:Humans; D006967:Hypersensitivity / Q000188:drug therapy* / Q000276:immunology / Q000378:metabolism; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology*; D007375:Interleukin-1 / Q000378:metabolism*; D007376:Interleukin-2 / Q000378:metabolism*; D007519:Isoantigens / Q000276:immunology*; D007962:Leukocytes / Q000187:drug effects / Q000378:metabolism; D007959:Lymphocyte Culture Test, Mixed; D051379:Mice; D008934:Mitogens / Q000494:pharmacology*; D051381:Rats; D013154:Spleen / Q000166:cytology / Q000378:metabolism; D013777:Tetrazoles / Q000494:pharmacology*
chemical_list: D001393:Azoles; D007211:Indoles; D007375:Interleukin-1; D007376:Interleukin-2; D007519:Isoantigens; D008934:Mitogens; D013777:Tetrazoles; C061320:CI 949