Pharmacological effects of cyclic nucleotides and their derivatives on tracheal smooth muscle

Szaduykis-Szadurski, L.; Weimann, G.; Berti, F.

doi:10.1016/0031-6989(72)90038-0

Cited by 13 publications

(1 citation statement)

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“…The nucleotide structure is unlikely to play a major role, since the majority of the active compounds are derivatives of cyclic GMP, which was shown to enhance .platelet aggregation induced by adrenaline or collagen; moreover, guanosine and guanine are unable to effect platelet function in vitro (Chiang et al 1976). The cyclic phosphate analogues might act by increasing cyclic AMP in platelets, as it has been shown in other tissues (Szaduykis-Szadurski et al 1972, Szaduykis-Szadurski and. In our experimental conditions, cyclic AMP level was unchanged in platelets when the derivatives were added to PRP alone or in association with compound RA233• Moreover, the derivatives were not able to potentiate the effect of PGE1 on cyclic AMP level.…”

Section: Discussionsupporting

confidence: 47%

Effect on Platelet Functions of Derivatives of Cyclic Nucleotides

et al. 1978

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SummaryDerivatives of cyclic nucleotides were evaluated for their ability to inhibit platelet aggregation and the release reaction. Derivatives substituted in position 8 (mainly 8-Br-cyclic GMP) were more active than 3’-5’ cyclic AMP, and their relative potency in inhibiting platelet aggregation and 14C-serotonin release was comparable to that of N62-0’-dibutyryl-cyclic AMP. Compounds substituted in position 6 or 2’-0 were not effective. The active compounds, which were also tested for their ability to stimulate platelet adenylate cyclase or to inhibit cyclic AMP phosphodiesterase, did not modify the intracellular levels of cyclic AMP. Since previous animal experiments have shown that these derivatives cause less side effects than cyclic AMP and its dibutyryl derivative in animals, it is suggested that modification of the cyclophosphate molecule might make it possible to find compounds active only on platelet function without interfering with other biological systems.

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Section: Discussionsupporting

confidence: 47%