Serotonergics, selective

Correlation between clinical effectiveness and receptor affinities, however, can be seen with other receptors in addition to the dopamine D2 receptor. These include other dopaminergic receptors, as well as noradrenergic and serotonergic receptors. For example, most antipsychotics also have high affinity for a -adrenoceptors and 5-HT2 receptors (225). Some antipsychotics have been shown to be selective for the adrenoceptor versus the a -adrenoceptor, for example, spiperone [749-02-0] (226) and risperidone (61) (221]... 

Tollefson GD, Montague-Clouse J, Tollefson SL Treatment of comorbid generalized anxiety in a recently detoxified alcohol population with a selective serotonergic drug (buspirone). J Clin Psychopharmacol 12 19-26, 1992... 

Reich DL, Silvay G Ketamine an update on the first twenty-five years of clinical experience. Can J Anaesth 36 186—197, 1989 Ricaurte GA, Forno LS, Wilson MA, et al (+/-)3,4-Methylenedioxymethamphetamine selectively damages central serotonergic neurons in nonhuman primates. JAMA 260 51-55, 1988... 

Lowry, CA, Odda, JE, Lightman, SL and Ingram, CD (2000) Corticotropin-releasing factor (CRF) increases the in vitro firing rates of serotonergic neurones in the rat dorsal raphe nucleus evidence for selective activation of a topographically organised mesolimbocortical system. J. Psychopharmacol. 14 (Suppl 2) All. 

Both these predictions are borne out by clinical experience despite the snag that only MAOb is found in serotonergic neurons (Saura et al. 1996). So far, there is no explanation for this anomaly. However, the lack of a tyramine-induced pressor effect with moclobemide probably owes more to the fact that it acts as a reversible inhibitor of MAOa (RIMA) than to its isoenzyme selectivity. Its reversible inhibition of MAOa means that, should tyramine ever accumulate in the periphery, it will displace... 

A related strategy would be to inactivate the 5-HTib/id autoreceptors which are found on serotonergic nerve terminals and so prevent feedback inhibition of 5-HT release in the terminal field. These drugs would not prevent the impact of indirect activation of 5-HTia receptors, and the reduced neuronal firing, by SSRIs (described above), but they would augment 5-HT release in the terminal field once the presynaptic 5-HTia receptors have desensitised. Selective 5-HTib/id antagonists have been developed only recently but will doubtless soon be tested in humans. 

Hervas, I, Raurich, A, Romero, L, Cortes, R and Artigas, F (1999) SSRI-induced functional changes in serotonergic neurones. In Selective Serotonin Reuptake Inhibitors (SSRIs) Past, Present and Future (Ed. Stanford, SC), RG Landes Co., Austin, TX, pp. 127-145. 

Ricaurte, G.A. Fomo, L.S. Wilson, M.A. DeLanney, L.E. Irwin, L. Molliver, M.E. and Langston, J.W. ( )-3,4-methylenedioxyamphetamine selectively damages central serotonergic neurons in nonhuman primates. 

Pharmacologic Profile of Amphetamine Derivatives at Various Brain Recognition Sites Selective Effects on Serotonergic Systems... 

Titeler. M. Lyon, R.A. Davis, K.A. and Glennon, R.A. Selectivity of serotonergic drugs for multiple brain serotonin receptors The role of H-DOB, a 5-HT2 agonist radioligand. Biochem Pharmacol 36 3265-3271,... 

This chapter discusses the responses of these extrapyramidal neuropeptide systems to the amphetamine analogs methamphetamine (METH), methylene dioxyamphetamine (MDA), and methylenedioxymethamphetamine (MDMA). These dmgs were selected for this study because they represent somewhat diverse mechanisms of action. While all three agents are able to enhance extrapyramidal serotonergic activity (Schmidt et al. 1987). only METH has been characterized as a substantial stimulant of the DA system. The effects of MDA and MDMA on extrapyramidal DA systems have not been well elucidated. Thus, evaluating and comparing the responses of the SP, NT, and Dyn extrapyramidal systems to these dmgs will help to determine the nature of the DA responses to METH, MDA, and MDMA administrations. 

Mamounas, L.A., and Molliver, M.E. Dual serotonergic projections to forebrain have separate origins in the dorsal and median raphe nuclei Retrograde transport after selective axonal ablation by p-chloroamphetamine (PCA). Abstr Soc Neurosci 13 907, 1987. 

O Heam, E. Battaglia, G. De Souza, E.B. Kuhar, M.J. and Molliver, M.E. Methylenedioxyamphetamine (MDA) and methylenedioxymethamphetamine (MDMA) cause selective ablation of serotonergic axon terminals in forebrain Immunocytochemical evidence for neurotoxicity. 

MAOI, monoamine oxidase inhibitor NaSSA, noradrenergic and specific serotonergic antidepressant NDRI, norepinephrine and dopamine reuptake inhibitor SARI, serotonin antagonist and reuptake inhibitor SNRI, serotonin and norepinephrine reuptake inhibitor SSRI, selective serotonin reuptake inhibitor TCA, tricyclic antidepressant. 

Fornal, C. A., Metzler, C. W., Gallegos, R. A. et al. (1996). WAY-100635, a potent and selective 5-hydroxytryptamineiA antagonist increases serotonergic neuronal activity in behaving cats Comparison with (S)-WAY-100635. J. Pharmacol. Exp. 

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