Evidence for a non-opioid sigma binding site in the guinea-pig myenteric plexus.
The presence of a binding site to (+)-(3H)SKF 10,047 was demonstrated in a guinea-pig myenteric plexus (MYP) membrane preparation. Specific binding to this receptor was saturable, reversible, linear with protein concentration and consisted of two components, a high affinity site (KD = 46 +/- 5 nM; Bmax = 3.4 +/- 0.5 pmole/g wet weight) and a low affinity site (KD= = 342 +/- 72 nM; Bmax = 22 +/- 3 pmole/g wet weight). Morphine and naloxone 10(-4) M were unable to displace (+)-(3H)SKF 10,047 binding. Haloperidol, imipramine, ethylketocyclazocine and propranolol were among the most potent compounds to inhibit this specific binding. These results suggest the presence of a non-opioid haloperidol sensitive sigma receptor in the MYP of the guinea-pig.
Roman
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F
JOUVEINAL Laboratoires, Fresnes, France.
Pascaud
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X
Vauché
D
D
Junien
J L
JL
D000818:Animals; D001667:Binding, Competitive; D002462:Cell Membrane / Q000378:metabolism; D002746:Chlorpromazine / Q000378:metabolism; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000378:metabolism; D016314:Ethylketocyclazocine; D006168:Guinea Pigs; D006220:Haloperidol / Q000378:metabolism; D007099:Imipramine / Q000378:metabolism; D008297:Male; D009197:Myenteric Plexus / Q000378:metabolism*; D010620:Phenazocine / Q000031:analogs & derivatives / Q000378:metabolism; D011433:Propranolol / Q000378:metabolism; D011957:Receptors, Opioid / Q000378:metabolism*; D017480:Receptors, sigma
D011957:Receptors, Opioid; D017480:Receptors, sigma; D016314:Ethylketocyclazocine; C012134:SK&F 10047; D011433:Propranolol; D010620:Phenazocine; D003496:Cyclazocine; D006220:Haloperidol; D007099:Imipramine; D002746:Chlorpromazine