Contractile effects of prostaglandin E2 in rat rectum: sensitivity to the prostaglandin antagonists diphloretin phosphate and SC 19220.
Prostaglandin E2 (PGE2) applied cumulatively (1 nM-1 microM) induced concentration-dependent tonic contractions in the longitudinal muscle of isolated rat rectum. The PGE2 effects were not altered by guanethidine (50 microM), whereas atropine (3 microM), guanethidine plus atropine or tetrodotoxin (0.1 microM) reduced them to an almost equal extent and increased the EC50 values for PGE2. The after-contractions following electrical stimulation were enhanced by PGE2 (10 nM) and inhibited by atropine. Diphloretin phosphate (DPP, 100 microM) shifted the regression lines for PGE2 to the right in both untreated and tetrodotoxin-treated preparations, and thereby increased the EC50 values. Slopes of the concentration-effect lines for PGE2 before and after DPP differed in the presence of tetrodotoxin. The regression line for PGE2 with SC 19220 (100 microM) in tetrodotoxin-treated preparations was shifted to the right in a parallel fashion. It is concluded that PGE2 exerted both a neural (cholinergic) and a smooth muscle effect. There may be a competitive antagonism between SC 19220 and PGE2 but the block by DPP may be nonselective.
Department of Experimental Pharmacology, Bulgarian Academy of Sciences, Sofia.
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Vassilev
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R
Radomirov
D000818:Animals; D001285:Atropine / Q000494:pharmacology; D012531:Dibenz(b,f)(1,4)oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-acetylhydrazide / Q000494:pharmacology*; D015232:Dinoprostone / Q000494:pharmacology*; D004558:Electric Stimulation; D006145:Guanethidine / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011121:Polyphloretin Phosphate / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012007:Rectum / Q000502:physiology*; D013779:Tetrodotoxin / Q000494:pharmacology
D012531:Dibenz(b,f)(1,4)oxazepine-10(11H)-carboxylic acid, 8-chloro-, 2-acetylhydrazide; C013509:diphloretin phosphate; D013779:Tetrodotoxin; D001285:Atropine; D011121:Polyphloretin Phosphate; D015232:Dinoprostone; D006145:Guanethidine