Pharmacological profile of a new pyrrolizine derivative inhibiting the enzymes cyclo-oxygenase and 5-lipoxygenase.
2,2-Dimethyl-6-(4-chlorophenyl)-7-phenyl, 2,3-dihydro-1H-pyrrolizine-5-yl)-acetic acid (ML 3000) is a dual inhibitor of the enzymes cyclo-oxygenase and 5-lipoxygenase in bovine and human thrombocytes and granulocytes. In animal experiments the compound has antiphlogistic, analgesic, antipyretic, antiasthmatic and antiaggregative activity at a dosage that causes no gastrointestinal damage.
Department of Drug Research, Merckle GmbH, Blaubeuren, Fed. Rep. of Germany.
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Laufer
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Tries
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Augustin
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Dannhardt
D000085:Acetates / Q000494:pharmacology*; D000818:Animals; D016718:Arachidonic Acid / Q000037:antagonists & inhibitors / Q000494:pharmacology; D001169:Arthritis, Experimental / Q000188:drug therapy; D016227:Benzoquinones; D001777:Blood Coagulation / Q000187:drug effects; D016084:Bronchoconstriction / Q000187:drug effects; D002351:Carrageenan; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology*; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D010147:Pain Measurement / Q000187:drug effects; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011758:Pyrroles / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D015002:Yeast, Dried
D000085:Acetates; D016227:Benzoquinones; D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors; D010975:Platelet Aggregation Inhibitors; D011758:Pyrroles; D016718:Arachidonic Acid; C029322:phenylbenzoquinone; D002351:Carrageenan; C088092:licofelone