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• W957221424 endingPage "50" @default.
• W957221424 startingPage "41" @default.
• W957221424 abstract "This chapter discusses the objectives to develop new anti-depressant drugs with fewer side effects and a rapid onset of action. Tricyclic compounds with antidepressant activity (TCAs), their therapeutic utility, biology, metabolism, and side effects also combined TCA-antipsychotic therapy was investigated. The influence of the seven-membered ring conformation of “6-7-6” TCAs and imine analogs of TCAs were studied of which the cyclopropa(c)cycloheptene derivatives were the most potent. Alprazolam, a benzodiazepine derivative with combined anti-anxiety–anti-depressant actions, was the most effective. Presynaptic α-blockade was noted only in molecules with an overall bent shape. “Second generation” antidepressants were discussed in the chapter. 2-C 6H5 CH2 C6H4 O(CH2)4 NHCH3 (MCI-2016) was one of the most potent members (0.78x amihptyline) of aminoalkoxyaryl compounds in a test for the prevention of reserpine-induced hypothermia in mice. Antidepressant actions were also produced by many bicyclic compounds. Foremost among these were 1,4-benzodiazepines and related structures that combine anti-anxiety and anti-depressant actions. A number of quinolines and related structures have antidepressant properties. The piperazinylquinoline DU 24565, a quipazine analog and 5-HT uptake inhibitor, is being studied as a potential antidepressant. Several ben-zodioxanylimidazoline apparently owe their antidepressant activity to blockade of central α2-adrenergic receptors. Anti-depressant effects have been associated with thyrotropin releasing hormone (TRH), pyroGlu-His-ProNH2, a peptide that potentiates the effects of imipramine on brain 5-HT systems. Monoamine oxidase inhibitors (MAOIs) investigations indicate greater anti-depressant efficacy for (+)-tranylcypromine, the more potent MAOI, than for the (-) isomer, a more effective uptake inhibitor. Central nervous system (CNS) stimulant effects of caffeine was recently correlated with their ability to bind to central adenosine (A1 and A2) receptors, thus preventing the depressant action of endogenous adenosine on nerve firing. ECS therapy, for which memory impairment is a major side effect, may find increased application in the future because new technologies are enhancing its precision, efficacy, and safety." @default.
• W957221424 created "2016-06-24" @default.
• W957221424 creator A5034688505 @default.
• W957221424 creator A5091366924 @default.
• W957221424 date "1982-01-01" @default.
• W957221424 modified "2023-09-25" @default.
• W957221424 title "Chapter 5. Antidepressants" @default.
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