Detail of "17318-31-9"

Reference

SQ 22536, an adenylate-cyclase inhibitor, prevents the antiplatelet effect of dazoxiben, a thromboxane-synthetase inhibitor

SQ 22536, an adenylate-cyclase inhibitor, prevents the antiplatelet effect of dazoxiben, a thromboxane-synthetase inhibitor. Bertele, Vittorio; Falanga, Anna; Tomasiak, Marian; Cerletti, Chiara; De Gaetano, Giovanni (Lab. Cardiovasc. Clin. Pharmacol., Ist. Ric. Farmacol. "Mario Negri", Milan, Italy). Thromb. Haemostasis, 51(1), 125-8 (English) 1984. CODEN: THHADQ. ISSN: 0340-6245. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 That dazoxiben (I) [78218-09-4], a selective inhibitor of thromboxane-A2-synthetase [60832-04-4] in human platelets, inhibited arachidonic acid-induced platelet aggregation in platelet-rich plasma samples from 4 out of 16 healthy volunteers. In these 4 responder samples, the anti-aggregating effect of dazoxiben was prevented by the compd. SQ 22536 [17318-31-9], a 9-substituted adenine analog, endowed with an inhibitory activity on adenylate-cyclase [9012-42-4].Several substances with their cas registry numbers 41598-07-6 and 60-92-4 may be metioned in this study. The compd. SQ 22536 also counteracted the antiaggregating effect of prostaglandin D2 [41598-07-6], a known activator of platelet adenylate-cyclase. When platelet thromboxane A2-synthetase was blocked by dazoxiben, a marked increase of prostaglandin D2 was concomitantly obsd. both in responder and nonresponder samples. The compd. SQ 22536 blunted the increase in platelet cAMP [60-92-4] caused by either dazoxiben and sodium arachidonate or prostaglandin D2. It is suggested that the antiaggregating effect of dazoxiben is mediated by newly synthesized prostaglandin D2. The latter acts by stimulating adenylate-cyclase and increasing cAMP levels. The compd. SQ 22536 prevents both phenomena. In nonresponder samples some factors, still to be defined, might counteract similarly to the compd. SQ 22536 the antiaggregating activity of PGD2. .

The effect of alkylxanthines and other phosphodiesterase inhibitors on adenosine-receptor mediated decrease in lipolysis and cyclic AMP accumulation in rat fat cells

The effect of alkylxanthines and other phosphodiesterase inhibitors on adenosine-receptor mediated decrease in lipolysis and cyclic AMP accumulation in rat fat cells. Fredholm, Bertil B.; Lindgren, Eva (Dep. Pharmacol., Karolinska Inst., Stockholm S-10401, Swed.). Acta Pharmacol. Toxicol., 54(1), 64-71 (English) 1984. CODEN: APTOA6. ISSN: 0001-6683. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Cyclic AMP [60-92-4] accumulation and glycerol [56-81-5] release were studied in isolated rat fat cells. Both processes were inhibited by R-site specific adenosine analogs such as -2-chloroadenosine [146-77-0], but poorly or not at all by the P-site selective analog SQ 22536 [17318-31-9]. The effect of a series of xanthine derivs. and of some structurally unrelated phosphodiesterase [9025-82-5] inhibitors as inhibitors of 2-chloroadenosine-induced inhibition of noradrenaline-stimulated cyclic AMP accumulation and lipolysis was examd. The 2-chloroadenosine effect on cyclic AMP accumulation was antagonized by several xanthines tested; the antilipolytic action of 2-chloroadenosine was also antagonized by these xanthines. The 2 potent phosphodiesterase inhibitors 7-benzyl-3-isobutylmethylxanthine [58481-23-5] and ZK 62711 [61413-54-5] were >20 times more potent as inhibitors of the antilipolytic effect of 2-chloroadenosine. Apparently, antagonism of a adenosine analog-induced antilipolytic effects is a convenient assay for adenosine antagonistic potency of drugs, except for drugs with a high potency as phosphodiesterase inhibitors. The lipolytic potency of the xanthine derivs. was also studied. The ability of the xanthines to stimulate basal and noradrenaline-stimulated lipolysis was generally in agreement with their potency as adenosine antagonists. Adenosine deaminase-induced lipolysis was stimulated by potent phosphodiesterase inhibitors.Except for chemicals metioned above, 1076-22-8 and 28822-58-4 are also used. .