Trends in Pharmacological Sciences
TIPS reviewBinding selectivity profiles for ligands of multiple receptor types: Focus on opioid receptors
References (18)
- et al.
Biochim. Biophys. Acta
(1975) - et al.
Life Sci.
(1981) - et al.
Eur. J. Pharmacol.
(1985) - et al.
J. Biol. Chem.
(1979) Am. J. Physiol.
(1948)- et al.
Mol. Pharmacol.
(1987) - et al.
Adv. Protein Chem.
(1976) - et al.
Br. J. Pharmacol.
(1982)
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Bioactivity studies on atypical natural opioid hexapeptides processed from proenkephalin (PENK) precursor polypeptides
2014, Comparative Biochemistry and Physiology Part - B: Biochemistry and Molecular BiologyCitation Excerpt :On the other hand the Ile6-hexapeptide exhibited high affinity at the DOP receptor (7 nM). Receptor type selectivity of the endogenous opioid peptides is generally less as compared to the highly specific synthetic ligands (Goldstein, 1987; Goldstein and Naidu, 1989). In addition, ligand selectivities determined experimentally depend on various factors, one of which is how many and how similar ligands and receptors there are.
Opioid μ-receptors as new target for insulin resistance
2013, Pharmacology and TherapeuticsCitation Excerpt :Subsequently, these subunits can inhibit adenylyl cyclases and thereby inhibit cAMP production and/or directly interact with different ion channels in the membrane (Pasternak, 1993). Extensive physiological, behavioral and pharmacological studies have defined at least three major types of opioid receptors designated μ, κ, and δ (Goldstein, 1987). These receptors are known to be widely distributed in the central nervous system (CNS) (Mansour et al., 1988).
Phylogenetic diversity and functional efficacy of the C-terminally expressed heptapeptide unit in the opioid precursor polypeptide proenkephalin A
2011, NeuroscienceCitation Excerpt :The receptor-type selectivity pattern (Table 2, last column) indicated that none of the compounds is highly specific for one particular receptor, although some preference for MOP and DOP receptors is observed. Selectivity of the endogenous opioids is generally less comparing to the highly specific synthetic ligands (Goldstein, 1987; Goldstein and Naidu, 1989). In addition, ligand selectivities determined experimentally depend on different factors, one of which is how many and how similar ligands and receptors there are.
Placenta ingestion by rats enhances δ- and κ-opioid antinociception, but suppresses μ-opioid antinociception
2004, Brain ResearchCitation Excerpt :The present series of experiments was designed to examine the contribution of each receptor separately by investigating the modulatory influence of ingested POEF on antinociception produced by independent central pharmacological activation of each of the three principal opioid receptor types. In each of the three experiments, placenta ingestion was combined with the intracerebroventricular (i.c.v.) injection of one of three different opioid receptor selective agonists: δ-preferring [d-Pen2,d-Pen5]enkephalin (DPDPE) [24,32,61]; μ-preferring [d-Ala2,N-MePhe4,Gly5-ol]enkephalin (DAMGO) [24,28,32]; or κ-preferring spiradoline [46,93]. In the present study, we hypothesized that placenta ingestion would enhance antinociception selectively induced at the δ-opioid receptor by DPDPE injection (Experiment 1), the μ-opioid receptor by DAMGO injection (Experiment 2), and the κ-opioid receptor by spiradoline injection (Experiment 3).
Evidence for changes in brain enkephalin contents associated to male rat sexual activity
2002, Behavioural Brain ResearchLoss of plasma glucose lowering response to cold stress in opioid μ-receptor knock-out diabetic mice
2001, Neuroscience Letters