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*Compound via MeSH
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*HALOPERIDOL
*N,N'-BIS(2-METHYLPHENYL)GUANIDINE

Characterization of specific (+)-[3H]N-allylnormetazocine and [3H]1,3- di(2-tolyl)guanidine binding sites in porcine gastric fundic mucosa

Y Harada, H Hara and T Sukamoto

Department of Pharmacology, Kanebo, Ltd., Osaka, Japan.

We have identified and characterized sigma receptor sites in porcine gastric fundic mucosa by receptor binding assay techniques using two highly selective radioligands of sigma receptor, (+)-[3H]N- allylnormetazocine (SKF 10,047) and [3H]1,3-di(2-tolyl)guanidine (DTG). Specific binding of (+)-[3H]SKF 10,047 and [3H]DTG in porcine gastric fundic mucosa were saturable, reversible and of high affinity and capacity with Kd: 90.5 nM, Bmax: 1058 fmol/mg of protein and Kd: 53.6 nM, Bmax: 3573.3 fmol/mg of protein, respectively. The inhibitory effects of sigma receptor ligands on specific (+)-[3H]SKF 10,047 binding decreased in the following order: haloperidol > DTG > or = (+)- 3-(3-hydroxyphenol)-N- (1-propyl)piperidine (3-PPP) > (+)-SKF 10,047 > (-)-3-PPP > or = dextromethorphan > rimcazole > (-)-SKF 10,047. Specific (+)-[3H]SKF 10,047 binding sites showed stereoselectivity for stereoisomers of SKF 10,047 and 3-PPP and were highly correlated with the profile of sigma-1 sites. On the other hand, the inhibitory effects on specific [3H]DTG binding decreased in the following order: DTG > haloperidol > rimcazole > (+)-3-PPP > or = (-)-3-PPP > dextromethorphan > (+)-SKF 10,047 = (-)-SKF 10,047. Specific [3H]DTG binding sites did not show stereoselectivity and were highly correlated with the profile of sigma-2 sites. These findings indicate that porcine gastric fundic mucosa contains sigma receptor sites with the characteristic of sigma-1 sites and sigma-like sites showing several of the characteristics of sigma-2 sites (putative sigma-2 sites).

Volume 269, Issue 3, pp. 905-910, 06/01/1994
Copyright © 1994 by American Society for Pharmacology and Experimental Therapeutics




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