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Establishing partial agonist activity at prostanoid IP(prostacyclin) receptorsRobert L. Jones

(Department of Pharmacology;Faculty of Medicine;The Chinese University of Hong Kong;Hong Kong SAR;China)

   Fifty years after the landmark work of R.P.Stephenson on the activity of alkytrimethylammonium salts on muscarinic receptors,partial agonism still fascinates both experimental and theoretical pharmacologists.In the prostanoid field,partial agonism has been reported for several non-prostanoid prostacyclin mimetics (EP 157,octimibate,BMY 45778).However,investigations are confounded by their high lipophilicity and the ability of some to inhibit PLC. Recently we observed that the prostacyclin analogue taprostene had a lower maximum response compared to cicaprost (usual IP standard agonist) on several smooth muscle preparations.Proving partial agonism was not possible due to the presence of highly sensitive EP_3 (contractile) or EP_4 (relaxant)……