Endocrine and receptor pharmacology of serotonergic anxiolytics, antipsychotics and antidepressants
Life SciencesPublished 1 January 1992
Andrew D. Levy, Louis D. Van de Kar
Citations72
SJR quartileQ1
SJR score1.31
SNIP1.07
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TL;DR
The receptor binding profiles of 5-HT anxiolytics, antipsychotics and antidepressants with their endocrine effects are compared to aid in understanding both the therapeutic and side effects of these drugs.
Abstract
Several classes of drugs that modify serotonin (5-HT) neurotransmission are either currently used, or are being evaluated for their potential use in the treatment of anxiety, schizophrenia, and depression. 5-HT1A agonists are considered potential anxiolytics, while some atypical antipsychotics are potent 5-HT2 antagonists (and also have modest dopamine D2 affinity). Furthermore, there is a diverse group of serotonergic drugs that may be effective antidepressants. Secretion of ACTH, corticosterone/cortisol, prolactin, renin, oxytocin and vasopressin are stimulated by activation of different 5-HT receptor subtypes, while other neurotransmitter receptors also influence the secretion of these hormones. We compared the receptor binding profiles of 5-HT anxiolytics, antipsychotics and antidepressants with their endocrine effects. These comparisons could aid in understanding both the therapeutic and side effects of these drugs.
Keywords
MedicineNeuroscienceBiochemistry, Genetics and Molecular Biology
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38 Citations1981David S. Cooper
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36 Citations1991Peter Roy‐Byrne, Deborah S. Cowley +4 more
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35 Citations1987J. Thomas Haskins, Eric A. Muth +1 more
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35 Citations1982Herbert Y. Meltzer, M. Simonovic +2 more
The ability of buspirone to block pituitary and striatal DA receptors is demonstrated and increased DA turnover in the striatum as measured by the AMPT-induced depletion of striatalDA levels.
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30 Citations1987David Nutt, Hugh Middleton +1 more
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30 Citations1989J. Frank Nash, Herbert Y. Meltzer
It is hypothesized that GEP and perhaps IPS are partial dopamine agonists which may contribute to their antianxiety and/or antidepressant properties.
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28 Citations1982Herbert Y. Meltzer, R. Fleming
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26 Citations1986Charles Saller, Andre I. Salama
Observations suggest that D-1 receptor stimulation can promote prolactin secretion and that low doses of SCH 23390 completely prevented the SKF 38393-induced elevations in plasma prol actin.
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The present data support the view that the mechanism of the anxiolytic action of buspirone is different from that of the benzodiazepines.
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European Journal of EndocrinologyAcute effects of medetomidine, a selective α2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man
22 Citations1988Antero Kallio, Markku Koulu +3 more
Medetomidine appears to resemble other alpha 2-adrenoceptor agonists, notably clonidine, in its endocrine effects, and its high selectivity and short duration of action make it a suitable tool for studies of the physiology and pharmacology ofalpha 2- adrenoceptors in man.
NeuropharmacologyThe effects of gepirone and 1-(2-pyrimidinyl)-piperazine on levels of corticosterone in rat plasma
21 Citations1989G.Keith Matheson, Deanna Gage-White +4 more
Results suggest that the increased levels of corticosterone, elicited by gepirone, were mediated through a serotonergic action rather than through noradrenergic activity, in the light of other work on the hypothalamic-pituitary-adrenal axis.
European Journal of PharmacologyGonadectomy changes the pituitaiy-adrenocortical response in mice to S-HT1A receptor agonists
21 Citations1991Toshio Matsuda, Yoshihide Nakano +3 more
The effects of 5-HT 1A receptor agonists such as 8-hydroxy-2-(ui-n-propylamino)tetralin (8-OH-DPAT), BP 554 and buspirone on the serum corticosterone level were significantly more pronounced in female than in male mice, and a similar sex difference was observed for the effect of 8-OH -DPAT on the piasma ACTH level.
PsychopharmacologyBenzodiazepine-induced sedation and cortisol suppression
20 Citations1992P. Christensen, Annette Lolk +2 more
The sedative and cortisol suppressing properties of oxazepam and nitrazepam were examined in eight healthy male subjects and the degree of sedation correlated significantly within drug groups with the concurrent benzodiazepine levels.
European Journal of PharmacologyTricyclic antidepressants activate the pituitary-adrenal axis in the rat. Tolerance to repeated drug administration
19 Citations1987Antonio Armario, C. García-Marquez
The effects of acute chronic administration of tricyclic antidepressants on the pituitary-adrenal axis were studied in adult male rats and the response of these rats to an acute dose of chlorimipramine was significantly lower than that of drug-naive rats, indicating tolerance to the drug.
Acta Psychiatrica ScandinavicaPharmacological data of the atypical neuroleptic compound melperone (Buronilr)
18 Citations1989Erik Christensson
Melperone is potent in blocking amphetamine induced locomotion, exploratory behaviour, L‐Dopa induced jumping and aggression suggesting a limbic mode of action and a weak effect of melperone on striatal DA neurotransmission.
Neuroscience & Biobehavioral Reviews5-HT-related drugs and human experimental anxiety
18 Citations1990Antônio Waldo Zuardi
It is suggested that the proanxiogenic effect of acute administration of 5- HT uptake inhibitors may be due to impaired 5-HT neurotransmission.
PsychoneuroendocrinologyProlactin control by the tubero-infundibular gabaergic system: role of anterior pituitary GABA receptors
18 Citations1984José Apud, C. Masotto +4 more
Failure of chronic treatment with aminooxyacetic acid, a GABA-T inhibitor, to modify the PRL-lowering effect of GABA-mimetic compounds, despite the decrease in the number of AP-GABA receptors, indicates that in normal conditions only a reduced number of receptors are operative.
Acta Pharmacologica et ToxicologicaEffect of Melperone, Two of its Metabolites and Thiothixene on Central Monoamine Metabolism and Prolactin Levels in Rodents
18 Citations1978Frits‐Axel Wiesel, L. Bjerkenstedt +1 more
Of two urinary metabolites ofmelperone investigated, one caused the same qualitative effects on monoamine metabolism as melperone itself but with reduced potency, and the other metabolite was ineffective.
British Journal of PharmacologySecretion of growth hormone elicited by intravenous desipramine in the conscious, unrestrained rat
17 Citations1991Maura Grealy, James M. O’Donnell
It is concluded that i.v. DMI caused an activation through indirect mechanisms of α2‐adrenoceptors specifically involved in hypothalamic‐pituitary regulation of GH release and also a distinct, independent and transient generalized activation of the pituitary-adrenal axis.
NeuroendocrinologyBrain Regulation of Renin Secretion Involves Central Histaminergic Neurons
17 Citations2008Steen Matzen, Ulrich Knigge +1 more
The results indicate that histaminergic neurons participate in the cerebral regulation of renin secretion and seem to exert a minor inhibiting effect on PRA via H1-receptors.
Biological PsychiatryGrowth hormone response to intravenous diazepam and placebo in 82 healthy men
16 Citations1990Maristela Monteiro, Marc A. Schuckit +3 more
Growth hormone response to placebo and two different doses of diazepam were evaluated in 82 healthy young men and there was a small but significant change in this hormone over time after placebo, but this was reflected by a slow rise following the saline infusion.
PsychopharmacologyLithium and 5-HT1A receptor sensitivity: a neuroendocrine study in healthy volunteers
16 Citations1991Annabel Walsh, Chris Ware +1 more
The results suggest that the ability of short-term lithium treatment to increase 5-HT-mediated neuroendocrine responses in humans is unlikely to be related to changes in the sensitivity of pre- or post-synaptic 5- HT1A receptors.
European Journal of PharmacologyRepeated treatment with the 5-HT1A receptor agonist, ipsapirone, does not affect 8-OH-DPAT- and stress-induced increases in plasma adrenaline levels in the rat
15 Citations1991Véronique Baudrie, Francis Chaouloff
The results indicate that 5-HT1A receptor-mediated activation of adrenaline release is not desensitised by short-term ipsapirone treatment, and the anxiolytic/antidepressant effect of ipsAPirone may not be explainable in terms of tolerance to some neuroendorinological consequences of stress.
Pharmacology & ToxicologyAmperozide – effect on prolactin release in the rat
12 Citations1990Agneta Albinsson, E. Eriksson +1 more
Results suggest that there is no direct effect of amperozide on the pituitary lactotrophs and that the attenuation of prolactin secretion in vivo is mediated at a higher level.
Endocrinology and Metabolism Clinics of North AmericaNeuroendocrine Findings in Anxiety Disorders
12 Citations1988George C. Curtis, Debra Glitz
A number of findings suggest receptor downregulation or enzyme induction of sorts that would be expected to mute or dampen these responses in anxiety disorders.
European Journal of PharmacologyS 14671: A novel naphthylpiperazane 5-HT1A agonist of high efficacy and exceptional in vivo potency
10 Citations1991Mark J. Millan, Hervé Canton +4 more
The novel, naphthylpiperazine 5-HT1A agonist, S 14671 (4-[(thenoyl-2)aminoethyl]-1-(7-methoxynaphtylpiperazine], displayed very high affinity for 5- HT1A binding sites and was about 10-fold more potent than 8-OH-DPAT and 100-foldMore potent than (+)-flesinoxan and buspirone in each test.
Hormone and Metabolic ResearchAcute Effects of Desipramine and Clomipramine on Pituitary-Adrenal Axis in Man
8 Citations1986W. R. HOLL, H. Fehm +3 more
Brain neurotransmitters play an essential role in central regula tion of hypothalamic factors which stimulate or inhibit the secretion of pituitary hormones, and the rise of both hormones following insulin-induced hypoglycemia was studied.
Endocrinology and Metabolism Clinics of North AmericaNeuroendocrine Findings in the Schizophrenias
8 Citations1988David L. Garver
The neuroendocrine windows for viewing brain function in the schizophrenias still permit indistinct images of the processes that modulate their release, and these images may provide important clues to the biopathology underlying these diseases.
Journal of Neural TransmissionThe neuroendocrine approach to psychiatric disorders: A critical appraisal
6 Citations1990E. E. M�ller
This contribution focuses upon the advantages and drawbacks of the neuroendocrine approach, caution and objectiveness necessary for the critical evaluation and interpretations of the data.
Life SciencesEffect of fluoxetine and metergoline on amphetamine-induced rise in plasma corticosterone
4 Citations1980Edward T. Knych, Richard M. Eisenberg
The hypothesis that the amphetamine-induced rise in plasma corticosterone is due, in part, to stimulation of serotonergic neurons is supported.
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