Opiate receptor interaction of a new analgesic drug 2-piperidinoethyl dibenzylglycolate.
The pharmacological properties of a new analgesic drug, 2-piperidinoethyl dibenzylglycolate (PDG), have been demonstrated by classical tests. The technique of iontophoresis was used in order to compare the effects of PDG with those of Tyr-D-Ser-Gly-Phe-Leu-Thr (DSTLE), syndyphalin, morphine and naloxone (NAL) on hypothalamic neurones. PDG as other four substances evoked only inhibitory responses. Some neurones, on which were tested three substances, were sensitive to one, two or three of these substances. The differential responses so obtained suggested that PDG does not act on mu- and delta-receptors but on an unidentified receptor for which morphine and NAL have a high affinity as agonist. Structural requirements for activity on different receptors were also proposed on the basis of crystallographic data and the above results.
Henichart
J P
JP
Carette
B
B
Bernier
J L
JL
Houssin
R
R
D000200:Action Potentials / Q000187:drug effects; D000700:Analgesics / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D004305:Dose-Response Relationship, Drug; D005260:Female; D006016:Glycolates / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D006168:Guinea Pigs; D007031:Hypothalamus / Q000502:physiology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D009474:Neurons / Q000187:drug effects; D009842:Oligopeptides / Q000494:pharmacology; D010880:Piperidines / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D011957:Receptors, Opioid / Q000378:metabolism*; D014961:X-Ray Diffraction
D000700:Analgesics; D006016:Glycolates; D009842:Oligopeptides; D010880:Piperidines; D011957:Receptors, Opioid; D009270:Naloxone; D009020:Morphine; C030776:syndyphalin; C045289:2-piperidinoethyl dibenzylglycolate