Antagonistic properties of four suramin-related compounds at vascular purine P2X receptors in the pithed rat.
The dose-response curve for the vasopressor effect of alpha, beta-methylene ATP in pithed rats was influenced by four suramin-related drugs (each at 100 mumol/kg). The curve was shifted to the right by a factor of 8 by 'compound 3' and by a factor of 2 by two other derivatives, but was not affected by the fourth analogue. Compound 3 had no effect on the vasopressor response to noradrenaline or neuropeptide Y. In conclusion, compound 3 is a purine P2X receptor antagonist which is approximately as potent as suramin, and which, like suramin, does not exhibit antagonistic properties at alpha-adrenoceptors and neuropeptide y receptors.
Urbanek
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E
Institut für Pharmakologie and Toxikologie, Universität Bonn, F.R.G.
Nickel
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P
Schlicker
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E
D000255:Adenosine Triphosphate / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D008297:Male; D009478:Neuropeptide Y / Q000494:pharmacology; D009638:Norepinephrine / Q000494:pharmacology; D058914:Purinergic Antagonists; D051381:Rats; D011919:Rats, Inbred Strains; D013498:Suramin / Q000031:analogs & derivatives*; D014662:Vasoconstrictor Agents / Q000494:pharmacology*
D009478:Neuropeptide Y; D058914:Purinergic Antagonists; D014662:Vasoconstrictor Agents; D013498:Suramin; D000255:Adenosine Triphosphate; C002630:alpha,beta-methyleneadenosine 5'-triphosphate; D009638:Norepinephrine