Pharmacological characteristics and distributions of sigma- and phencyclidine receptors in the animal kingdom.
The phylogenetic distributions of sigma- and phencyclidine receptors in neural tissues of 13 species and the pharmacological characteristics of these receptors in whole sea anemone and neural tissues of the guinea pig, chicken, and frog were studied. Specific binding of [3H]haloperidol and [3H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine, ligands that bind with high affinity to sigma- and phencyclidine receptors, respectively, was detected in all organisms examined. The order of potencies of various ligands to inhibit 1 nM [3H]haloperidol binding in brains of frogs and guinea pigs or 1 nM [3H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine in chicken or guinea pig brain homogenates was very similar. However, the characteristics and stereospecificity of binding of the two radioligands in sea anemone were different than in higher organisms. The results suggest that sigma- and phencyclidine binding sites are evolutionarily old, as the characteristics of the two sites are well preserved over a range of vertebrate phyla.
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Addiction Research Center, National Institute on Drug Abuse, Baltimore, MD 21224.
Weissman
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London
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D000818:Animals; D001665:Binding Sites; D002645:Chickens; D005399:Fishes; D006168:Guinea Pigs; D006220:Haloperidol / Q000378:metabolism; D008297:Male; D010622:Phencyclidine / Q000031:analogs & derivatives / Q000378:metabolism; D010802:Phylogeny; D011898:Ranidae; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D011957:Receptors, Opioid / Q000378:metabolism*; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; D012453:Saimiri; D012615:Sea Anemones; D014426:Turtles
D017981:Receptors, Neurotransmitter; D011957:Receptors, Opioid; D017478:Receptors, Phencyclidine; D017480:Receptors, sigma; C012058:tenocyclidine; D010622:Phencyclidine; D006220:Haloperidol