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N-methyl-D-aspartate receptor-mediated contractions of the guinea pig ileum longitudinal muscle/myenteric plexus preparation: modulation by phencyclidine and glycine receptors.
J Pharmacol Exp Ther. 1991 May; 257(2):754-66.JP

Abstract

Glutamate evoked contractions of the longitudinal muscle/myenteric plexus (LMMP) preparation by an action at N-methyl-D-aspartate (NMDA) receptors. Other agonists at the NMDA recognition site, but not quisquilate or kainate, also contracted the LMMP, and glutamate-evoked contractions were competitively inhibited by selective NMDA receptor antagonists. Glutamate-evoked contractions were noncompetitively inhibited by MK-801 [(+)-5-methyl-10,11-dihydro-5H-dibenzo-[a,d]cyclohepten-5,10-imine moleate], phencyclidine (PCP) and other compounds that bind to the PCP receptor, which is a binding site on the NMDA channel complex. Their potencies for this effect were highly correlated with their affinities for the PCP receptor. Glycine significantly shifted the glutamate concentration-response curve to the left. Glycine site antagonists caused a glycine-sensitive, noncompetitive inhibition of glutamate-evoked contractions, and their potencies for this effect were highly correlated with their affinities for the glycine binding site of the NMDA channel complex. Mg++ and Zn++ also noncompetitively inhibited glutamate-evoked contractions. The modulatory effects of glycine, Mg++, Zn++ and PCP receptor ligands were specific to glutamate-evoked contractions. MK-801 was highly selective for inhibition of glutamate-evoked contractions; MK-801 also inhibited nicotinic responses at a 500-fold lower potency. Two novel compounds are described that bind to the PCP receptor with high affinity and selectively inhibit glutamate-evoked contractions in the LMMP.

Authors+Show Affiliations

Department of Physiology, Oregon Health Sciences University, Portland.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

1674535

Citation

Campbell, B G., et al. "N-methyl-D-aspartate Receptor-mediated Contractions of the Guinea Pig Ileum Longitudinal Muscle/myenteric Plexus Preparation: Modulation By Phencyclidine and Glycine Receptors." The Journal of Pharmacology and Experimental Therapeutics, vol. 257, no. 2, 1991, pp. 754-66.
Campbell BG, Couceyro P, Keana JF, et al. N-methyl-D-aspartate receptor-mediated contractions of the guinea pig ileum longitudinal muscle/myenteric plexus preparation: modulation by phencyclidine and glycine receptors. J Pharmacol Exp Ther. 1991;257(2):754-66.
Campbell, B. G., Couceyro, P., Keana, J. F., & Weber, E. (1991). N-methyl-D-aspartate receptor-mediated contractions of the guinea pig ileum longitudinal muscle/myenteric plexus preparation: modulation by phencyclidine and glycine receptors. The Journal of Pharmacology and Experimental Therapeutics, 257(2), 754-66.
Campbell BG, et al. N-methyl-D-aspartate Receptor-mediated Contractions of the Guinea Pig Ileum Longitudinal Muscle/myenteric Plexus Preparation: Modulation By Phencyclidine and Glycine Receptors. J Pharmacol Exp Ther. 1991;257(2):754-66. PubMed PMID: 1674535.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - N-methyl-D-aspartate receptor-mediated contractions of the guinea pig ileum longitudinal muscle/myenteric plexus preparation: modulation by phencyclidine and glycine receptors. AU - Campbell,B G, AU - Couceyro,P, AU - Keana,J F, AU - Weber,E, PY - 1991/5/1/pubmed PY - 1991/5/1/medline PY - 1991/5/1/entrez SP - 754 EP - 66 JF - The Journal of pharmacology and experimental therapeutics JO - J Pharmacol Exp Ther VL - 257 IS - 2 N2 - Glutamate evoked contractions of the longitudinal muscle/myenteric plexus (LMMP) preparation by an action at N-methyl-D-aspartate (NMDA) receptors. Other agonists at the NMDA recognition site, but not quisquilate or kainate, also contracted the LMMP, and glutamate-evoked contractions were competitively inhibited by selective NMDA receptor antagonists. Glutamate-evoked contractions were noncompetitively inhibited by MK-801 [(+)-5-methyl-10,11-dihydro-5H-dibenzo-[a,d]cyclohepten-5,10-imine moleate], phencyclidine (PCP) and other compounds that bind to the PCP receptor, which is a binding site on the NMDA channel complex. Their potencies for this effect were highly correlated with their affinities for the PCP receptor. Glycine significantly shifted the glutamate concentration-response curve to the left. Glycine site antagonists caused a glycine-sensitive, noncompetitive inhibition of glutamate-evoked contractions, and their potencies for this effect were highly correlated with their affinities for the glycine binding site of the NMDA channel complex. Mg++ and Zn++ also noncompetitively inhibited glutamate-evoked contractions. The modulatory effects of glycine, Mg++, Zn++ and PCP receptor ligands were specific to glutamate-evoked contractions. MK-801 was highly selective for inhibition of glutamate-evoked contractions; MK-801 also inhibited nicotinic responses at a 500-fold lower potency. Two novel compounds are described that bind to the PCP receptor with high affinity and selectively inhibit glutamate-evoked contractions in the LMMP. SN - 0022-3565 UR - https://www.unboundmedicine.com/medline/citation/1674535/N_methyl_D_aspartate_receptor_mediated_contractions_of_the_guinea_pig_ileum_longitudinal_muscle/myenteric_plexus_preparation:_modulation_by_phencyclidine_and_glycine_receptors_ DB - PRIME DP - Unbound Medicine ER -