Monoamine oxidase inhibitors inhibit [3H]quinpirole binding in rat striatal membranes
| Autor: | Errol B. DeSouza, D. E. Grigoriadis, Beth Levant |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Male
Monoamine Oxidase Inhibitors Quinpirole Apomorphine medicine.drug_class Monoamine oxidase Dopamine Agents In Vitro Techniques Pharmacology Binding Competitive Rats Sprague-Dawley Iproniazid Phenazocine Clorgyline medicine Animals Receptors sigma Ergolines Monoamine Oxidase Monoamine oxidase inhibitor Membranes Receptors Dopamine D2 Chemistry Pargyline Corpus Striatum Rats Kinetics Monoamine neurotransmitter Spiperone Antidepressant medicine.drug |
| Zdroj: | European Journal of Pharmacology: Molecular Pharmacology. 246:171-178 |
| ISSN: | 0922-4106 |
| DOI: | 10.1016/0922-4106(93)90095-q |
| Popis: | This study describes interactions of monoamine oxidase inhibitors at binding sites labeled by [3H]quinpirole, a putatively selective ligand for dopamine D2-like receptors, in in vitro binding assays in rat brain. Monoamine oxidase inhibitors potently and competitively inhibited equilibrium binding of [3H]quinpirole in homogenate binding assays with the following rank order of potencies: clorgyline ⩾ Ro 41-1049 > pargyline > (−)-deprenyl > (+)-deprenyl > Ro 16-6491 > iproniazid. This rank order of potencies does not correlate with the potencies of these drugs at monoamine oxidase-A or monoamine oxidase-B, σ site(s) or dopamine receptors. Monoamine oxidase inhibitors did not alter the ability of quinpirole to compete for [3H]spiperone binding. Quinpirole did not inhibit monoamine oxidase-A or monoamine oxidase-B activity and had low affinity (200 nM) for σ site(s). These data suggest a potential novel binding site for [3H]quinpirole in rat brain and/or an alternative site of action for the antidepressant effects of monoamine oxidase inhibitors. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|