Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action.
Article Details
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Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K
Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action.
Biol Psychiatry. 1984 Sep;19(9):1283-91.
- PubMed ID
- 6149771 [ View in PubMed]
- Abstract
The relative potencies of a variety of neuroleptic drugs and antidepressant agents in competing for the binding of 3H-clonidine and 3H-yohimbine to alpha 2-adrenergic receptors of the rat cerebral cortex were quantified. The rank order of potencies of neuroleptics tested in competing for both ligand bindings is: clocapramine, carpipramine much greater than perphenazine, fluphenazine, alpha,beta-flupentixol greater than propericiazine, levomepromazine greater than chlorpromazine, pimozide greater than moperone much greater than haloperidol, sulpiride. Among the antidepressants, mianserin is the most potent antidepressant. Amitriptyline has a substantial affinity, while desipramine, imipramine, and clomipramine are the least potent. It is concluded that a number of neuroleptics and antidepressant agents display a potent or moderate affinity to alpha 2-receptor sites. These findings support the suggestion that some neuroleptics enhance the release of norepinephrine (NE) mainly by acting on presynaptic alpha 2-receptors, and that the alpha 2-receptor blocking property may have an important role in the mechanism of the antidepressant effect of some neuroleptic compounds.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Methotrimeprazine Alpha-2A adrenergic receptor Protein Humans UnknownAntagonistDetails Methotrimeprazine Alpha-2B adrenergic receptor Protein Humans UnknownAntagonistDetails Methotrimeprazine Alpha-2C adrenergic receptor Protein Humans UnknownAntagonistDetails Periciazine Alpha-2A adrenergic receptor Protein Humans YesAntagonistDetails