Specificity of opioids towards the μ-, δ- and ϵ-opiate receptors

@article{Wster1979SpecificityOO,
  title={Specificity of opioids towards the $\mu$-, $\delta$- and ϵ-opiate receptors},
  author={Michael W{\"u}ster and Rüdiger Schulz and Albert Herz},
  journal={Neuroscience Letters},
  year={1979},
  volume={15},
  pages={193-198}
}
Abstract The potency of a number of opioid agonists has been determined on three different bioassays, the isolated guinea-pig ileum (GPI), the mouse vas deferens (MVD) and the rat vas deferens (RVD). With the exception of β-endorphin, compounds with opioid activity on the GPI and the MVD exhibited considerably less or no activity on the RVD; the opiate receptor in this latter tissue being thus characterized as β-endorphin selective (‘ϵ-receptor’). A system of classification of opioids according… 
The direction of opioid agonists towards μ-, δ- and ε-receptors in the vas deferens of the mouse and the rat
Abstract Chronic treatment of mice with specific opioids results in the development of tolerance of particular opiate receptors in the mouse vas deferens (MVD). Accordingly, the infusion of animals
μ-, δ-, κ-Opioid receptors and their subtypes. A critical review with emphasis on radioligand binding experiments
TLDR
The signal transduction pathways, structure, and brain and spinal cord localization of the established subtypes (mu, delta, kappa), and evidence suggesting heterogeneity of these subtypes, in particular from radioligand binding studies, is discussed critically.
Opiate activity and receptor selectivity of dynorphin1–13 and related peptides
TLDR
None of the dynorphin-related peptides tested displayed a pronounced opiate-like antinociception when administered intracerebroventricularly into rats.
Are there subtypes (isoreceptors) of multiple opiate receptors in the mouse vas deferens?
TLDR
The hypothesis of heterogeneity of opiate receptors was tested with the electrically stimulated mouse vas deferens and found that opioids classified as mu-receptor agonists do not necessarily exhibit cross-tolerance to each other, and this gives rise to an interpretation which may postulate the existence of subtypes (isoreceptors) of the already known opiates receptors.
Non-peptide δ opioid agonists and antagonists
Following a flurry of medicinal chemistry activity in the late 1980s, a number of non-peptide pharmacological tools, selective for the δ opioid receptors, became available to challenge the
Differential effect of humoral endorphin on the binding of opiate agonists and antagonists.
TLDR
Humoral (H) endorphin, a novel endogenous factor with opiate-like activity was further characterized using various radioreceptor assays and a multisite model of the opiate receptor is presented.
Opioid Receptors: Types, Distribution, and Pharmacological Profiles
Although the use of opium can be traced back to the ancient Sumerians [1] and the receptor theory of drug actions was proposed at the turn of the century [2], the actual postulation and demonstration
Comparative study on the effect of morphine and the opioid-like peptides in the vas deferens of rodents: species and strain differences, evidence for multiple opiate receptors.
TLDR
The guinea pig vas deferens has apparently lost the sensitivity to the inhibitory influence of the opioids, suggesting the absence of μ or δ opiate receptors in this tissue.
A subclassification of multiple opiate receptors by means of selective tolerance development.
TLDR
Tests with isolated tissue preparations made highly tolerant in vivo to the mu-agonist morphine proved that these were of almost unchanged sensitivity to different types of receptor agonists such as kappa-agonists, indicating that the ability to selectively induce tolerance on particular types of opiate receptors represents a reliable tool for the differentiation and characterization of multiple opiates receptors.
Diprenorphine has agonist activity at opioid kappa-receptors in the myenteric plexus of the guinea-pig ileum.
TLDR
The opioid agonist and antagonist activities of diprenorphine have been tested in four in vitro bioassay preparations and in the guinea-pig ileum it is an antagonist at mu-receptors and an agonist at kappa-receptorors.
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 12 REFERENCES
OPIOID AGONISTS AND ANTAGONISTS: ACTION ON MULTIPLE OPIATE RECEPTORS
TLDR
Results from binding studies performed on rat vas deferens homogenates parallelled the data obtained from the isolated preparation and the high antagonistic activity of various narcotic antagonists was very similar on both preparations.
Selective receptors for β-endorphin on the rat vas deferens
Abstract The isolated rat vas deferens, being insensitive to morphine, contains selective binding sites for β-end-orphin. A half-maximal inhibition of twitch tension evoked by electrical stimulation
Multiple opiate receptors
TLDR
Whether the complex effects of opioid peptides are mediated by single or multiple types of opiate receptors is discussed.
Endogenous opioid peptides: multiple agonists and receptors
TLDR
It is concluded that the opioid peptidergic system has agonists of different characteristics which interact with more than one type of receptor.
ASSESSMENT IN THE GUINEA‐PIG ILEUM AND MOUSE VAS DEFERENS OF BENZOMORPHANS WHICH HAVE STRONG ANTINOCICEPTIVE ACTIVITY BUT DO NOT SUBSTITUTE FOR MORPHINE IN THE DEPENDENT MONKEY
1 Four benzomorphans which have potent antinociceptive activity in the hot‐plate and writhing tests in the mouse but do not suppress or precipitate withdrawal symptoms in the morphine‐dependent
Inactivity of narcotic glucuronides as analgesics and on guinea-pig ileum.
TLDR
Results support the conclusion that analgesia seen after intracerebral injection of levorphanol-3-glucuronide is caused by the free base resulting from hydrolysis in vivo.
The effects of adrenaline, noradrenaline and isoprenaline on inhibitory α‐ and β‐adrenoceptors in the longitudinal muscle of the guinea‐pig ileum
1 Two preparations, a segment of the ileum and the myenteric plexus‐longitudinal muscle preparation, have been used for an analysis of the inhibitory effects of adrenaline, noradrenaline and
Evidence for two separate opiate peptide neuronal systems
WHEN Hughes et al.1 first described the sequences of the enkephalins, they pointed out that methionine–enkephalin (met-enkephalin) could be found in β-lipotropin (β-LPH 61–65). The entire C-terminal
Regional dissociation of beta-endorphin and enkephalin contents in rat brain and pituitary.
TLDR
The results show that brain endorphin levels are independent of pituitary endorphIn levels; they suggest that beta-endorphin-containing neurons and those containing enkephalin constitute two separate groups of brain cells.
...
1
2
...