Effects of buflomedil and its two derivatives, CRL40634 and CRL40598, on pancreatic exocrine secretion in the rat.
Buflomedil is a vasoactive drug used in the treatment of peripheral vascular disease, and seems to be an antagonist of both alpha 1- and alpha 2-vascular adrenoceptors. CRL40634 and CRL40598 are metabolites of buflomedil and also possess vasoactive properties. The purpose of this study was to investigate whether buflomedil, CRL40634 and CRL40598 have antagonist activity on the alpha 2-adrenoceptors involved in the inhibition of exocrine pancreatic secretion. In acute pancreatic fistula rats, buflomedil, CRL40634 and CRL40598 did not suppress the inhibitory effect of clonidine against 2-deoxy-glucose-induced pancreatic secretion. However, all three drugs inhibited 2-deoxy-glucose-induced pancreatic secretion, their order of potency being CRL40598 greater than CRL40634 greater than buflomedil.
Chariot
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INSERM U 239, Faculté de Médecine Xavier Bichat, Paris, France.
Nagain
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Vaille
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Rozé
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D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D001639:Bicarbonates / Q000378:metabolism; D003000:Clonidine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D003847:Deoxyglucose / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D010179:Pancreas / Q000187:drug effects / Q000378:metabolism*; D010189:Pancreatic Juice / Q000378:metabolism; D011506:Proteins / Q000378:metabolism; D011759:Pyrrolidines / Q000494:pharmacology*; D051381:Rats; D012964:Sodium / Q000378:metabolism; D014665:Vasodilator Agents / Q000494:pharmacology*
D001639:Bicarbonates; D011506:Proteins; D011759:Pyrrolidines; D014665:Vasodilator Agents; C063624:CRL 40598; C063625:CRL 40634; D003847:Deoxyglucose; D012964:Sodium; D003000:Clonidine; D000109:Acetylcholine; C010651:buflomedil