[Anti-inflammatory property of 6-chloro-5-cyclohexyl-1-indancarboxylic acid (TAI-284) (author's transl)]. 1977

H Fujimura, and K Tsurumi, and M Nozaki, and K Kyuki

Anti-inflammatory activity and the mode of action of TAI-284 were investigated in animal models and compared with the activities of indomethacin. TAI-28 inhibited the increased vascular permeability in rats and mice which is the primary stage of inflammatory process, but the activity was less than that of indomethacin. The compound was as active as indomethacin in inhibiting acute rat paw edema induced by carrageenin and fracture. Furthermore, in the inhibitory effects on ultraviolet erythema in guinea pigs, durable paw edema induced by mustard and wound healing in rats, TAI-284 showed the same or more potent activity than indomethacin. Therefore, TAI-284 proved to have the same anti-inflammatory activity as indomethacin. TAI-284 protected rabbits from sudden death caused by intravenous injection of arachidonic acid, but the activity was about one twentieth less than that of indomethacin. The anti-inflammatory action of TAI-284 was derived from the mode of action of non-steroidal anti-inflammatory drugs, judging from the effects on ultraviolet erythema and death by arachidonic acid. On the other hand, the compound was more potent on secondary or thema and death by arachidonic acid. On the other hand, the compound was more potent on secondary or late stage than on primary stage of inflammation, and to some extent showed the mode of action seen with steroid antiinflammatory drugs. TAI-284 displayed marked inhibitory activity on nystatin induced paw edema in rats. It is suggested that the antinflammatory action of TAI-284 may be due to the lysosomal stabilizing effect.

UI MeSH Term Description Entries
D007189 Indans Aryl CYCLOPENTANES that are a reduced (protonated) form of INDENES. Indanones
D007192 Indenes A family of fused-ring hydrocarbons isolated from coal tar that act as intermediates in various chemical reactions and are used in the production of coumarone-indene resins.
D007213 Indomethacin A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D008297 Male Males
D002199 Capillary Permeability The property of blood capillary ENDOTHELIUM that allows for the selective exchange of substances between the blood and surrounding tissues and through membranous barriers such as the BLOOD-AIR BARRIER; BLOOD-AQUEOUS BARRIER; BLOOD-BRAIN BARRIER; BLOOD-NERVE BARRIER; BLOOD-RETINAL BARRIER; and BLOOD-TESTIS BARRIER. Small lipid-soluble molecules such as carbon dioxide and oxygen move freely by diffusion. Water and water-soluble molecules cannot pass through the endothelial walls and are dependent on microscopic pores. These pores show narrow areas (TIGHT JUNCTIONS) which may limit large molecule movement. Microvascular Permeability,Permeability, Capillary,Permeability, Microvascular,Vascular Permeability,Capillary Permeabilities,Microvascular Permeabilities,Permeabilities, Capillary,Permeabilities, Microvascular,Permeabilities, Vascular,Permeability, Vascular,Vascular Permeabilities
D003645 Death, Sudden The abrupt cessation of all vital bodily functions, manifested by the permanent loss of total cerebral, respiratory, and cardiovascular functions. Sudden Death
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004487 Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE. Dropsy,Hydrops,Anasarca
D004890 Erythema Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes. Erythemas
D005260 Female Females

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