TRIMU-5, a μ2-opioid receptor agonist, stimulates the hypothalamo-pituitary-adrenal axis

@article{Eisenberg1994TRIMU5A,
  title={TRIMU-5, a $\mu$2-opioid receptor agonist, stimulates the hypothalamo-pituitary-adrenal axis},
  author={R. Eisenberg},
  journal={Pharmacology Biochemistry and Behavior},
  year={1994},
  volume={47},
  pages={943-946}
}
  • R. Eisenberg
  • Published 1 April 1994
  • Chemistry
  • Pharmacology Biochemistry and Behavior
Previous work in our laboratory has shown that DAMGO (ICV) will cause an elevation in plasma corticosterone (CS). The effect was blocked by pretreatment with beta-FNA but not by naloxonazine, suggesting indirectly that DAMGO's effect was via a mu 2-opioid receptor. TRIMU-5, a mu 2 agonist/mu 1 antagonist, was tested in a similar series of experiments to show more directly that the effect of DAMGO to increase plasma CS was via the mu 2 receptor. Experiments were conducted on conscious… Expand
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References

SHOWING 1-10 OF 26 REFERENCES
DAMGO stimulates the hypothalamo-pituitary-adrenal axis through a mu-2 opioid receptor.
  • R. Eisenberg
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1993
TLDR
DAMGO, a highly selective mu opioid agonist, is capable of stimulating the hypothalamo-pituitary-adrenal (HPA) axis to produce a dose-related elevation in plasma corticosterone (CS), and which of the mu receptors was involved using naloxonazine, a mu-1 receptor-selective antagonist was confirmed. Expand
Effects of naltrexone on plasma corticosterone in opiate-naive rats: a central action.
TLDR
Results obtained demonstrate that NTX has a similar effect on plasma corticosterone as NX at the appropriate doses and that the effect is a central rather than a peripheral one. Expand
Effects of selective opioid-receptor blockade on the hypothalamo-pituitary-adrenocortical responses to surgical trauma in the rat.
TLDR
The results suggest that mu- and kappa-opioid receptors mediate opposing actions of endogenous opioid peptides, both of which may be physiologically important in the regulation of CRF release. Expand
Plasma corticosterone changes in response to central or peripheral administration of kappa and sigma opiate agonists.
  • R. Eisenberg
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1985
TLDR
Data support the notion that stimulation of several subclasses of opiate receptors will result in the activation of the hypothalamo-pituitary-adrenal axis and appear that the mu opiate receptor is involved in the initiation of acute opiate dependence. Expand
Kappa opiate agonists modulate the hypothalamic-pituitary-adrenocortical axis in the rat.
TLDR
Systemic injections of opiate agonists were made in male rats to elucidate the involvement of multiple opioid receptors in the stress response, confirming a mu and delta opioid input into the hypothalamic-pituitary-adrenocortical axis. Expand
mu-receptor mediates elevated glucose and corticosterone after third ventricle injection of opioid peptides.
TLDR
Results imply that mu-opioid binding sites previously identified in central autonomic regions may be involved in the regulation of circulating glucose and corticosterone. Expand
Effects of naloxone on plasma corticosterone in the opiate-naive rat.
TLDR
The results suggest that NX may have a direct effect on opiate receptors resulting in an elevation of plasma hormone levels or NX may be disrupting an endogenous opiate-receptor interaction producing a stress response. Expand
Analgesic potency of TRIMU-5: A mixed μ2 opioid receptor agonists/μ1 opioid receptor antagonist
TRIMU-5 (Try-D-Ala-Gly-NH-(CH2)2CH(CH3)2) is a potent enkephalin analog with analgesic actions. Detailed studies show high affinity for both μ1 and μ2 sites, with poor affinity for σ, ν1 and ν3Expand
μ-, δ-, κ- and ϵ-Opioid receptor modulation of the hypothalamic-pituitary-adrenocortical (HPA) axis: subchronic tolerance studies of endogenous opioid peptides
In opiate-naive rats, the endogenous opioid peptides, beta-endorphin, dynorphin(1-13) and Met-Enk-Arg-Phe (MEAP) and the synthetic enkephalin analogue D-Ala2-D-Leu5-Enk (DADLE) potently stimulatedExpand
Effects of acute and chronic administration of μ- and δ-opeoid agonists on the hypothalamic-pituitary-adrenocortical (HPA) axis in the rat
Abstract The control of hypothalamic-pituitary-adrenocortical (HPA) activity by opioids seems to involve stimulatory and inhibitory pathways. The purpose of the present study was to determine theExpand
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