In vivo studies with low doses of levocabastine and diphenhydramine, but not pyrilamine, antagonize neurotensin-mediated antinociception.

The present study describes in vivo experiments in the rat addressing the role of levocabastine, and two other specific histamine H1 antagonists, diphenhydramine and pyrilamine, at neurotensin (NT)-mediated hypothermia and antinociception (hotplate). Levocabastine given i.p.

Pharmacological profile of antidepressants and related compounds at human monoamine transporters.

Using radioligand binding assays, we determined the equilibrium dissociation constants (KD's) for 37 antidepressants, three of their metabolites (desmethylcitalopram, desmethylsertraline, and norfluoxetine), some mood stabilizers, and assorted other compounds (some antiepileptics, Ca2+ channel antagonists, benzodiazepines, psychostimulants, antihistamines, and monoamines) for the human serotonin, norepinephrine, and dopamine transporters. Among the compounds that we tested, mazindol was the most potent at the human norepinephrine and dopamine transporters with KD's of 0.45 +/- 0.

The expression of mRNA for a kappa opioid receptor in the substantia nigra of Parkinson's disease brain.

We molecularly cloned the kappa opioid receptor from a human substantia nigra cDNA library. When expressed in HEK293 cells, the cloned receptor had similar pharmacological characteristics to the rat kappa opioid receptor. Northern blot analysis showed the presence of a single transcript of about 6 kb in size for mRNA prepared from the substantia nigra.

Characterization of the genomic structure, promoter region, and a tetranucleotide repeat polymorphism of the human neurotensin receptor gene.

In the present study, we have cloned the human neurotensin receptor (NTR) gene, determined its structure, demonstrated that its promoter is functional in transfection experiments, and identified the start site of transcription and a tetranucleotide repeat polymorphism that locates at less than 3 kilobase pairs from the gene. The gene contains three introns, all in the coding regions. Several differences in genomic clones and previously characterized cDNA sequences are reconciled.

Proposed ligand binding site of the transmembrane receptor for neurotensin(8-13).

We report here the first proposed ligand binding site of the transmembrane receptor for neurotensin(8-13) in human and rat, the corresponding bound conformation of the peptide ligand, and site-directed mutagenesis studies that support the binding site model. These three-dimensional structures were generated by using a heuristic approach in conjunction with experimental data. The proposed neurotensin(8-13) binding site is primarily composed of eight residues (i.