Reference

The role of leukotrienes in ocular inflammation

The role of leukotrienes in ocular inflammation. 2. The effect of anti-SRS-A substance (KC-404) on experimental uveitis in guinea pigs. Sunada, Akinobu; Kin, Keien; Narumi, Chikako; Mizutani, Toshiko; Miyanaga, Yoshitaka (Tokyo Women's Med. Coll., Daini Hosp., Tokyo, Japan). Nippon Ganka Gakkai Zasshi, 88(11), 1341-9 (Japanese) 1984. CODEN: NGZAA6. ISSN: 0029-0203. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) KC-404 [50847-11-5], an antagonist of anaphylactic slow-reacting substances, administered to guinea pigs with uveitis had anti-inflammatory effects comparable to those of indomethacin and steroids. However, at a dose equiv. to 1/10 the clin. dosage (or 1.82 mg/mL), KC-404 was more effective than was indomethacin.

A new vasodilator 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine (KC-404) has a dual mechanism of action on platelet aggregation

A new vasodilator 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine (KC-404) has a dual mechanism of action on platelet aggregation. Ohashi, M.; Okubo, H.; Kito, J.; Nishino, K. (Cent. Res. Lab., Kyorin Pharm. Co., Ltd., Tochigi 329-01, Japan). Arch. Int. Pharmacodyn. Ther., 283(2), 321-34 (English) 1986. CODEN: AIPTAK. ISSN: 0003-9780. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) KC-404 (I) [50847-11-5] at a concn. of 34.34 ′ 10-5 M inhibited ADP-, arachidonic acid- and collagen-induced aggregation of rabbit platelets. In rabbit, KC-404 (0.5 and 2mg/kg, i.v.) caused a decrease in wt. of collagen strip extracorporeally superfused with arterial blood, because of a disaggregation of deposited platelet aggregates. This disaggregatory effect of KC-404 was markedly diminished by the pretreatment of animals with aspirin. KC-404 (34.34 ′ 10-6 M) and its major metabolite diOH-KC-404 [101162-42-9] (33.78 ′ 10-7 M) potentiated the anti-aggregatory action of prostacyclin [35121-78-9] on rabbit platelets. KC-404 (34.34 ′10-8 M) exerted a similar effect in rat platelets. KC-404 had no significant effect on 6-keto-PGF1a and thromboxane A2 formation by rat aortic segment and rabbit platelets, resp. KC-404 inhibited cAMP phosphodiesterase [9036-21-9] (Ki = 91 mM). The present results indicate that KC-404 exhibits its anti-platelet effect via the inhibition of cAMP phosphodiesterase activity in platelets and via the potentiation of anti-aggregatory activity of prostacyclin on platelets.Except for chemicals metioned above, 101162-42-9 and 35121-78-9 are also used. .