Role of Endogenous Opioid Receptor Agonists in Regulation of Heart Resistence to the Arrhythmogenic Action of Short-Term Ischemia and Reperfusion

2005 ◽  
Vol 139 (2) ◽  
pp. 172-175 ◽  
Author(s):  
L. N. Maslov ◽  
Yu. B. Lishmanov ◽  
N. V. Naryzhnaya ◽  
E. V. Budankova ◽  
D. L. Stakheev ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Ischemia And Reperfusion ◽  
Short Term ◽  
Endogenous Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists

Dilemma of Addiction and Respiratory Depression in the Treatment of Pain: A Prototypical Endomorphin as a New Approach

Pain Medicine ◽  
2019 ◽  
Vol 21 (5) ◽  
pp. 992-1004 ◽  
Author(s):  
Lynn Webster ◽  
William K Schmidt
Keyword(s):  
Side Effects ◽  
Respiratory Depression ◽  
Opioid Receptor ◽  
Severe Pain ◽  
Mu Opioid Receptor ◽  
Endogenous Opioid Peptides ◽  
Endogenous Opioid ◽  
Mu Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists

Abstract Objective Although mu-opioid receptor agonists have been the mainstay of analgesic regimens for moderate to severe pain, they are associated with serious side effects, risks, and limitations. We evaluate the most serious risks associated with conventional opioids and compare these with the pharmacology of CYT-1010, a prototypical endomorphin and mu-opioid receptor agonist. Results Addiction and respiratory depression are serious risks of traditional mu-opioid analgesics. Mitigation strategies have been inadequate at addressing the opioid crisis and may interfere with the effective treatment of pain. Improved understanding of mu-opioid receptor biology and the discovery in 1997 of an additional and unique family of endogenous opioid peptides (endomorphins) have provided a pathway for dissociating analgesia from opioid-related adverse events and developing new classes of mu-opioid receptor agonists that use biased signaling and/or target novel sites to produce analgesia with reduced side effect liability. Endomorphin-1 and -2 are endogenous opioid peptides highly selective for mu-opioid receptors that exhibit potent analgesia with reduced side effects. CYT-1010 is a cyclized, D-lysine-containing analog of endomorphin-1 with a novel mechanism of action targeting traditional mu- and exon 11/truncated mu-opioid receptor 6TM variants. CYT-1010 preclinical data have demonstrated reduced abuse potential and analgesic potency exceeding that of morphine. In an initial phase 1 clinical study, CYT-1010 demonstrated significant analgesia vs baseline and no respiratory depression at the dose levels tested. Conclusions CYT-1010 and other novel mu-opioid receptor agonists in clinical development are promising alternatives to conventional opioids that may offer the possibility of safer treatment of moderate to severe pain.

Agonists of endogenous opioid peptides suppress LH, and stimulate cortisol and growth hormone during the follicular phase in heifers

1989 ◽  
Vol 121 (1) ◽  
pp. 11-17 ◽  
Author(s):  
J. D. Armstrong ◽  
B. H. Johnson
Keyword(s):  
Opioid Receptor ◽  
Physiological Saline ◽  
Inhibitory Effect ◽  
Follicular Phase ◽  
Endogenous Opioid ◽  
Receptor Agonists ◽  
Prostaglandin F ◽  
Induced Changes ◽  
Opioid Receptor Agonists ◽  
Angus Heifers

ABSTRACT We evaluated the effects of [d-Ala2,Me,Phe4,Met(0)ol]-enkephalin (FK 33-824) and morphine, opioid receptor agonists, on concentrations of LH, cortisol and GH during the follicular phase in heifers. During three trials, oestrous cycles of Angus heifers were synchronized by two injections of prostaglandin F2α (PGF2α) resulting in 17 induced follicular phases over an 80-day period. Treatments were administered 24 h after the second injection of PGF2α. Blood samples were collected at 15-min intervals from 3 h before until 5 h after i.v. administration of 2 ml physiological saline (trials 1, 2 and 3), 0·5 mg morphine/kg (trials 1 and 2) or 1·8 μg FK 33-824/kg (trials 1 and 2) or 6·7 μg FK 33-824/kg (trial 3). Administration of both doses of FK 33-824 and morphine inhibited episodic release of LH for approximately 60 min. The concentration of cortisol was increased (P<0·05) after both doses of FK 33-824, but was unaffected (P>0·5) by morphine or saline. The serum concentration of GH was increased (P<0·01) after both doses of FK 33-824 or morphine, but saline was without effect. These results provide evidence of an inhibitory effect of opioid receptor agonists on LH (FK 33-824 and morphine) and a stimulatory effect on cortisol (FK 33-824) and GH (FK 33-824 and morphine) during the follicular phase in heifers. Divergent effects of morphine and FK 33-824 on cortisol observed in this study provide evidence that opioid-induced changes in LH, GH and cortisol result from activation of different opioid receptors. Journal of Endocrinology (1989) 121, 11–17

The role of opioid receptor agonists in ischemic preconditioning

2013 ◽  
Vol 720 (1-3) ◽  
pp. 401-408 ◽  
Author(s):  
Stylianos Dragasis ◽  
Eleni Bassiakou ◽  
Nicoletta Iacovidou ◽  
Louiza Papadimitriou ◽  
Petter Andreas Steen ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Ischemic Preconditioning ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists
Sign in / Sign up

Export Citation Format

Share Document