This paper is only available as a PDF. To read, Please Download here.
Abstract
The effects of MK-212 ¦6-chloro-2-(1-piperazinyl)-pyrazine¦ (10, 20, and 40 mg. orally).
a centrally acting serotonin (5-HT) receptor agonist and placebo, on serum cortisol,
prolactin, and growth hormone levels were studied in eight healthy men over 3-hr.
MK-212 produced a dose-related increase in serum cortisol levels, with the 20- and
40-mg doses producing significant elevations. Serum prolactin levels were significantly
elevated only by the 40-mg dose. Serum GH levels were not significantly modified by
any dose of MK-212. The cortisol and prolactin responses to the 40-mg dose of MK-212
were positively correlated (rho = + 0.85, p < 0.02). MK-212 was generally well tolerated by the subjects. Headache and nausea were observed
at the higher doses, but did not appear to be related to the increase in serum cortisol
and prolactin levels. MK-212 may stimulate the secretion of cortisol and prolactin
in humans via a serotonin (5-HT2) receptor mechanism and may be a valuable tool with
which to study 5-HT receptor sensitivity in humans.
To read this article in full you will need to make a payment
Purchase one-time access:
Academic & Personal: 24 hour online accessCorporate R&D Professionals: 24 hour online accessOne-time access price info
- For academic or personal research use, select 'Academic and Personal'
- For corporate R&D use, select 'Corporate R&D Professionals'
Subscribe:
Subscribe to Biological PsychiatryAlready a print subscriber? Claim online access
Already an online subscriber? Sign in
Register: Create an account
Institutional Access: Sign in to ScienceDirect
References
- Evidence that 5-HT agonist-induced rotational behavior in the rat is mediated via 5-HT1 receptors.Psychopharmacology. 1984; 83: 163-165
- Psychoendocrinology and growth hormone: A review.Psychoneuroendocrinology. 1978; 3: 131-153
- Serotonin function in anxiety II. Effects of the serotonin agonist mCPP in panic disorder patients and healthy subjects.Psychopharmacology. 1987; 92: 14-24
- MK-212: A serotonin-like agonist in the CNS.Gen Pharmacol. 1979; 10: 287-290
- Discriminative stimulus properties of the serotonin agonist MK-212.Psychopharmacology. 1986; 90: 193-197
- Serotonergic stimulation of pituitary-adrenocortical function in rats.Neuroendocrinology. 1981; 32: 118-127
- Central serotonin antagonist activity of ketanserin.Res Commun Chem Pathol Pharmacol. 1984; 46: 151-154
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents.Life Sci. 1984; 35: 2505-2511
- Serotonergic function in depression. Prolactin response to intravenous tryptophan in depressed patients and healthy subjects.Arch Gen Psychiatry. 1984; 41: 398-402
- Characterization of a novel 3H-5-hydroxytryptamine binding site subtype in bovine brain membranes.J Neurosci. 1987; 7: 894-903
- Stimulation of corticosterone and β-endorphin secretion in the rat by selective 5-HT receptor subtype activation.Eur J Pharmacol. 1987; 137: 1-8
- A biochemical and neuroendocrine study of the Serotonergic system in depression.in: Hippius I New Results in Depression Research. Springer-Verlag, New York1986: 169-188
- Serotonergic stimulation of adrenocorticotropin secretion in man.J Clin Endocrinol Metab. 1984; 58: 458-462
- 5-Hydroxytryptamine (5-HT) dependent myoclonus in guinea pigs is induced through brainstem 5-HT1 receptors.Neurosci Lett. 1984; 44: 241-246
- Serotonin and mood: Neuroendocrine aspects.in: Current Topics in Neuroendocrinology. vol 8. Springer-Verlag, Heidelberg1987 (in press).
- Neuroendocrine effects of psychotomimetic drugs.McLean Hosp J VI. 1981; 2: 115-136
- Effect of serotonin precursors and serotonin agonists on plasma hormone levels.in: Ho BT Serotonin in Biological Psychiatry. Raven Press, New York1982: 117-139
- The effect of buspirone on prolactin and growth hormone secretion in man.Arch Gen Psychiatry. 1983; 40: 1099-1102
- Effect of 5-hydroxytryptophan on scrum cortisol levels in major affective disorders. I. Enhanced response in depression and mania.Arch Gen Psychiatry. 1984; 41: 366-374
- Serotonergic stimulation of pituitary-adrenocortical activity in rats: Evidence for multiple sites of action.Life Sci. 1984; 34: 1891-1898
- Neuroendocrine effects of M-chlorophenylpiperazine, a serotonin agonist, in humans.J Clin Endocrinol Metab. 1985; 61: 1179-1184
- Neuroendocrine effects of quipazine in man in healthy state or with neurological disorders.J Neural Transmiss. 1980; 47: 273-297
- Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors.Biol Psychiatry. 1985; 20: 971-979
- Multiple serotonin receptors and their physiological significance.in: Fed Proc. 42. 1983: 213-217
- Plasma prolactin changes following fenfluramine in depressed patients compared to controls: An evaluation of central serotonergic responsivity in depression.Life Sci. 1984; 34: 1029-1039
- Determination of selective and nonselective compounds for the 5-HT1A and 5-HT1B receptor subtypes in rat frontal cortex.J Pharmacol Exp Ther. 1984; 231: 480-487
- A comparative electrophysiological and biochemical assessment of serotonin (5-HT) and a novel 5-HT agonist (MK-212) on central serotonergic receptors.Neuropharmacology. 1984; 23: 1271-1277
Article info
Publication history
Received in revised form:
August 21,
1987
Received:
March 31,
1987
Identification
Copyright
© 1988 Published by Elsevier Inc.
