Phencyclidine receptors and N-methyl-D-aspartate antagonism: electrophysiologic data correlates with known behaviours.
Pharmacology, biochemistry, and behavior October 1, 1988 DOI: 10.1016/0091-3057(88)90346-2 via PubMed
Summary
AI-generated from the abstractA series of psychoactive phencyclidine (PCP) and sigma receptor ligands were compared for their ability to block NMDA receptors using cortical wedges and isolated frog spinal cords. Phencyclidine receptor ligands, but not sigma or kappa ligands, selectively antagonized NMDA on both preparations. Combination studies suggested that dissociative anaesthetics and sigma benzomorphans act at the same site. The relative potencies of the drugs as NMDA antagonists correlated well with their potency in PCP receptor binding studies in vitro and in PCP discrimination studies in vivo.
Study at a glance
| Characteristics | Laboratory study Peer reviewed |
|---|---|
| Population | Cortical wedges and isolated frog spinal cords |
| Intervention | phencyclidine (PCP) and sigma receptor ligands |
| Key finding | Phencyclidine receptor ligands, but not sigma or kappa ligands, are selective NMDA antagonists, and their potencies correlate with PCP receptor binding and discrimination studies. |
Abstract
Using cortical wedges and isolated frog spinal cords, the potency of a series of psychoactive phencyclidine (PCP) and sigma receptor ligands as antagonists of N-methyl-D-aspartate (NMDA) has been compared with their potency in neurochemical and behavioural studies. Phencyclidine receptor, but not sigma or kappa, ligands were selective antagonists of NMDA on both preparations. Combination studies suggested that dissociative anaesthetics and sigma benzomorphans act at the same site. The relative potencies of the drugs as NMDA antagonists correlated well with their potency in PCP receptor binding studies in vitro and in PCP discrimination studies in vivo.