Unknown

Dataset Information

0

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.

ABSTRACT: Enkephalin analogues with a 4-anilidopiperidine scaffold have been designed and synthesized to achieve therapeutic benefit for the treatment of pain due to mixed mu and delta opioid agonist activities. Ligand 16, in which a Dmt-substituted enkephalin-like structure was linked to the N-phenyl-N-piperidin-4-yl propionamide moiety, showed very high binding affinities (0.4 nM) at mu and delta receptors with an increased hydrophobicity (aLogP = 2.96). This novel lead compound was found to have very potent agonist activities in MVD (1.8 nM) and GPI (8.5 nM) assays.

SUBMITTER: Lee YS 

PROVIDER: S-EPMC2678914 | biostudies-literature | 2007 Nov

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.

Lee Yeon Sun YS   Petrov Ravil R   Park Chad K CK   Ma Shou-wu SW   Davis Peg P   Lai Josephine J   Porreca Frank F   Vardanyan Ruben R   Hruby Victor J VJ  

Journal of medicinal chemistry 20071010 22

Enkephalin analogues with a 4-anilidopiperidine scaffold have been designed and synthesized to achieve therapeutic benefit for the treatment of pain due to mixed mu and delta opioid agonist activities. Ligand 16, in which a Dmt-substituted enkephalin-like structure was linked to the N-phenyl-N-piperidin-4-yl propionamide moiety, showed very high binding affinities (0.4 nM) at mu and delta receptors with an increased hydrophobicity (aLogP = 2.96). This novel lead compound was found to have very p  ...[more]

Similar Datasets

Unknown Enkephalin Disinhibits Mu Opioid Receptor-Rich Striatal Patches via Delta Opioid Receptors.
| S-EPMC4698909 | biostudies-literature
Unknown The Meta-Position of Phe4 in Leu-Enkephalin Regulates Potency, Selectivity, Functional Activity, and Signaling Bias at the Delta and Mu Opioid Receptors.
| S-EPMC6943441 | biostudies-literature
Unknown Coexpression of delta- and mu-opioid receptors in nociceptive sensory neurons.
| S-EPMC2919913 | biostudies-literature
Unknown Contribution of mu and delta opioid receptors to the pharmacological profile of kappa opioid receptor subtypes.
| S-EPMC4086711 | biostudies-literature
Unknown Heteromerization of the μ- and δ-opioid receptors produces ligand-biased antagonism and alters μ-receptor trafficking.
| S-EPMC3097170 | biostudies-literature
Unknown Functional independence of endogenous μ- and δ-opioid receptors co-expressed in cholinergic interneurons.
| S-EPMC8718112 | biostudies-literature
Unknown Convergent, functionally independent signaling by mu and delta opioid receptors in hippocampal parvalbumin interneurons.
| S-EPMC8716102 | biostudies-literature
Unknown Kappa but not delta or mu opioid receptors form homodimers at low membrane densities.
| S-EPMC8629795 | biostudies-literature
Unknown Mu and delta opioid receptors play opposite nociceptive and behavioural roles on nerve-injured mice.
| S-EPMC7042108 | biostudies-literature
Unknown Interaction and regulatory functions of μ- and δ-opioid receptors in nociceptive afferent neurons.
| S-EPMC5560394 | biostudies-other