title: Bremazocine differentially antagonizes responses to selective mu and delta opioid receptor agonists in rat hippocampus.
abstract: The effects of mu, delta and kappa opioid receptor agonists were examined on evoked field potentials in brain slices prepared from rat hippocampus. The effects of the mu-selective opioid peptide [D-Ala2, NMe-Phe4, Met(O)5ol]enkephalin (FK 33-824) and the delta-selective peptide [D-Pen2, D-Pen5]enkephalin (DPDPE) were qualitatively and quantitatively similar. Both increased the amplitude of evoked population spike responses when perfused in low nanomolar concentrations in a fashion consistent with what has been previously reported for other opiate agonists such as morphine. The kappa-selective agonists bremazocine and U-50, 488H were without effect upon evoked responses at concentrations as high as 10 microM. Bremazocine, but not U-50, 488H, proved to be an extremely potent antagonist of responses to both mu- and delta- selective agonists. Moreover, bremazocine was considerably more potent in antagonizing responses to FK 33-824 than DPDPE, which supports the hypothesis that FK 33-824 and DPDPE act via different receptors. Thus, although bremazocine is an agonist at kappa receptors, it appears to act as an antagonist at other opioid receptor sites.
mesh_terms: D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology*; D005405:D-Ala(2),MePhe(4),Met(0)-ol-enkephalin / Q000494:pharmacology; D004558:Electric Stimulation; D004566:Electrodes; D020881:Enkephalin, D-Penicillamine (2,5)-; D004745:Enkephalins / Q000494:pharmacology; D006624:Hippocampus / Q000187:drug effects / Q000502:physiology*; D066298:In Vitro Techniques; D008297:Male; D009019:Morphinans / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects* / Q000502:physiology; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu
chemical_list: D001575:Benzomorphans; D004745:Enkephalins; D009019:Morphinans; D011759:Pyrrolidines; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D005405:D-Ala(2),MePhe(4),Met(0)-ol-enkephalin; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D020881:Enkephalin, D-Penicillamine (2,5)-; C027248:bremazocine