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Biomedical subjects

R B Rothman

Publications and source records attributed to R B Rothman.

258 records · Page 15Linked to original sources
PubMedDate not supplied

PCP site 2: a high affinity MK-801-insensitive phencyclidine binding site.

Phencyclidine (PCP), a psychotomimetic drug with anticonvulsant and neuroprotective properties interacts with several central nervous system (CNS) macromolecules. These include cholinergic receptors, potassium channels, biogenic amine reuptake systems, the N-methyl-D-aspartate (NMDA) excitatory amino acid receptor, and sigma binding sites. The good correlation between the affinity of arylcycloalkylamines for high affinity PCP binding sites and their ED50 values for inhibition of [3H]dopamine uptake supports the notion that a PCP binding site associated with the transporter for the biogenic amines should be detectable in ligand binding studies. This article reviews data primarily from the author's laboratory, which shows that the PCP analog, [3H]1-[1-(2-thienyl)cyclohexyl]piperidine, binds to a second site, not associated with the NMDA receptor/ionophore complex, called PCP site 2. The ligand-selectivity of this binding site and the evidence that it is associated with the biogenic amine transporters are reviewed.

Animals↗
PubMedDate not supplied

Effect of dopamine receptor antagonists on cocaine subjective effects: a naturalistic case study.

Schizophrenic patients on neuroleptic medications abuse cocaine and report cocaine-induced euphoria. This study was undertaken to provide better clinical characterization of these phenomena by administering the POMS and a custom-designed questionnaire. A group of heavy cocaine users who were not mentally ill served as the control group. The results clearly suggest that schizophrenic patients report cocaine-induced euphoria and post-use craving despite being treated with therapeutic doses of haloperidol or fluphenazine. The responses of the control group were similar to that of the schizophrenic group except that the latter subjects reported a greater degree of anxiety. These results suggest that blockade of D2 receptors is not sufficient to block cocaine-induced subjective effects in humans.

Adult↗
PubMedDate not supplied

Binding surface analysis: an intuitive yet quantitative method for the design and analysis of ligand binding studies.

Ligand binding techniques are widely used to measure drug, hormone, and neurotransmitter receptors. Despite its wide application, quantitative methods of data analysis have not been widely adopted. This paper reviews some of the problems associated with semiquantitative methods of data analysis, and describes a mathematically based approach to the design and analysis of ligand binding experiments. Widely spaced concentrations of radiolabeled ligand are displaced by concentrations of cold drug. Analysis of these curves, which describe a "binding surface," with computer curve-fitting programs significantly increases the power of the ligand-binding technique.

Animals↗