Binding of antidepressants to human brain receptors: focus on newer generation compounds

摘要: Using radioligand binding assays and postmortem normal human brain tissue, we obtained equilibrium dissociation constants (Kds) for 17 antidepressants two of their metabolites at histamine H1, muscarinic, α1-adrenergic, α2-adrenergic, dopamine D2, serotonin 5-HT1A, 5-HT2 receptors. Several newer were compared with older drugs. In addition, studied some antimuscarinic, antiparkinson, antihistamine, neuroleptic compounds these For the antidepressants, classical tricyclic most potent drugs five seven receptors (all but α2-adrenergic 5-HT1A receptors). The chlorophenylpiperazine derivative (etoperidone, nefazodone, trazodone) Of ten antihistamines tested, none was more than doxepin H1 At muscarinic had a range potencies, which mostly weaker those antimuscarinics. From in vitro data, expect adinazolam, bupropion, fluoxetine, sertraline, tomoxetine, venlafaxine not to block any vivo. An antidepressant's potency blocking specific receptor is predictive certain side effects drug-drug interactions. These studies can provide guidelines clinician choice antidepressant.