MK-212 increases rat plasma ACTH concentration by activation of the 5-HT1C receptor subtype

  title={MK-212 increases rat plasma ACTH concentration by activation of the 5-HT1C receptor subtype},
  author={B. H. King and Celia Brazell and Colin T. Dourish and Derek N. Middlemiss},
  journal={Neuroscience Letters},
The effects of the serotonin agonist MK-212, on rat plasma ACTH were examined. MK-212 significantly increased plasma ACTH levels, and this effect was blocked by the 5-HT1C antagonists mesulergine and metergoline but not by spiperone, ketanserin, or (-)-pindolol. The results suggest that MK-212 activates the 5-HT1C receptor subtype to increase ACTH. 
Effect of cocaine injections on the neuroendocrine response to the serotonin agonist MK-212
The data indicate that a wide-spectrum 5-HT (serotonin) agonist such as MK-212 can reveal differential neuroendocrine responses that could be related to cocaine-induced changes in the different 5- HT receptor subtypes that regulate the secretion of these hormones. Expand
Effect of pindolol pretreatment on MK-212-induced plasma cortisol and prolactin responses in normal men
The data suggest that the MK-212-induced cortisol response may be mediated by 5-HT2A or 5 -HT2C receptor activation, or both, despite 5- HT1A inhibition; however, PRL secretion by MK- 212 requires 5-ht1A receptor availability as well as 5-Hat2A/5- HT2C receptors activation, since blockade of the former appears to blunt the PRL responses to MK-211. Expand
Inhibitory effect of ritanserin on the 5-hydroxytryptophan-mediated cortisol, ACTH and prolactin secretion in humans
Oral administration of the serotonin (5-HT) precursorl-5-hydroxytryptophan, 200 mg, significantly increased plasma cortisol levels in man and a borderline effect of 5-HTP on plasma ACTH levels was found. Expand
Effect of pindolol on thel-5-htp-induced increase in plasma prolactin and cortisol concentrations in man
It is suggested that thel-5-HTP-induced increase in PRL but not cortisol secretion requires 5-HT1A receptor activation, and the implication of this synergistic effect for interpretation of neuroendocrine studies involving the serotonergic system in man is discussed. Expand
Involvement of 5-HT2A receptors in the elevation of rat serum corticosterone concentrations by quipazine and MK-212.
It is suggested that 5-HT2A receptors rather than 5- HT2C receptors mediate the serum corticosterone increases by both quipazine and MK-212. Expand
The 5-HT2 Receptor Agonist MK-212 Reduces Food Intake and Increases Resting but Prevents the Behavioural Satiety Sequence
Temporal analysis is an essential tool in understanding of drug induced anorexia because the lack of appearance of the Behavioural Satiety Sequence is more similar to a state of hyper-sedation than to DOI induced hyper-activity. Expand
Neuroendocrine effects of sumatriptan
The present data cannot exclude the possibility that the neuroendocrine changes of sumatriptan reflect non-specific stress responses or changes in pituitary blood flow, and may be a consequence of selective activation of 5- HT1D or 5-HT1B receptors. Expand
Repeated cocaine modifies the neuroendocrine responses to the 5-HT1C/5-HT2 receptor agonist DOI.
The data suggest that 5-HT2 receptor-mediated responses for ACTH, corticosterone and prolactin secretion become supersensitive following repeated cocaine, which is likely a consequence of deficits in the function of 5- HT nerve terminals. Expand
Antagonism of Serotonin Agonist-Elicited Increases in Serum Corticosterone Concentration in Rats
Serum corticosterone and adrenocorticotropin (ACTH) concentrations are increased in rats by numerous direct-acting and indirect-acting serotonin receptor agonists. Antagonism of these increases byExpand
Comparison of the potency of MDL 100,907 and SB 242084 in blocking the serotonin (5-HT)2 receptor agonist-induced increases in rat serum corticosterone concentrations: evidence for 5-HT2A receptor mediation of the HPA axis
These findings implicate 5-HT(2A) receptors rather than 5-ht(2C) receptors in mediating increases in rat serum corticosterone produced by direct-acting 5- HT(2) receptor agonists in vivo. Expand


Stimulation of corticosterone and beta-endorphin secretion in the rat by selective 5-HT receptor subtype activation.
It is concluded that stimulation of either 5-HT1A or5-HT2 receptors results in an activation of the hypothalamic-pituitary-adrenal axis in the rat. Expand
Differential effects of serotonin (5-HT1A and 5-HT2) agonists and antagonists on renin and corticosterone secretion.
The data suggest that 5- HT1A receptors do not play a role in the regulation of renin secretion, whereas stimulation of 5-HT2 receptors enhances renin release. Expand
Stimulation of serum cortisol and prolactin secretion in humans by MK-212, a centrally active serotonin agonist
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. Expand
Selective desensitization of serotonin (5-HT) receptor-mediated hyperthermia by mianserin and other 5-HT antagonists
It is concluded that there is a selective decrease in the responsiveness of the 5-HT2 receptors mediating MK-212-induced hyperthermia, 48 hr after a single injection of mianserin or other selected5-HT antagonists. Expand
Functional correlates of serotonin 5-HT1 recognition sites.
  • D. Hoyer
  • Biology, Medicine
  • Journal of receptor research
  • 1988
It is shown that functional correlates do indeed exist for subtypes of 5-HT1 recognition sites; moreover, these are markedly different from the effects mediated by 5- HT2 (5-HT D) or 5 -HT3 (5 -HT M) receptors. Expand
Evidence that mCPP may have behavioural effects mediated by central 5‐HT1C receptors
As mianserin, cyproheptadine and mesulergine in the absence of mCPP did not increase locomotion but increased the number of feeding scores, the activation of 5‐HT1C‐receptors may be of physiological importance in the control of appetite. Expand
Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1c) receptors.
It is concluded that quipazine and MK-212 are partial agonists at 5-HT-2 receptors in cerebral cortex, whereas 1-NP, TFMPP and MCPP are pure antagonists of the cortical 5- HT-2 receptor. Expand
The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site.
The kinetic and pharmacological characteristics of the binding of ligands to frontal cortex and hippocampus demonstrated the presence of 5-HT1 and5-HT2 sites in both tissues, although hippocampus was richer in 5-ht1 (subtype 5- HT1A) sites. Expand