A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability

Bioorganic & Medicinal Chemistry Letters
2006.0

Abstract

Buprenorphine analogs have been synthesized. In the studies of analgesic and addictive effects in mice and [(35)S]GTPgammaS binding assay in human brain tissue, an analog of buprenorphine where the tert-butyl is replaced by a cyclobutyl moiety (16) has been identified as a selective kappa-partial agonist which gives antinociceptive effects, but has low abuse potential. The results may lead to lower degrees of dysphoria than full kappa-agonists.

Knowledge Graph

Similar Paper

A highly selective κ-opioid receptor agonist with low addictive potential and dependence liability
Bioorganic & Medicinal Chemistry Letters 2006.0
Structural Determinants of Opioid and NOP Receptor Activity in Derivatives of Buprenorphine
Journal of Medicinal Chemistry 2011.0
High-affinity carbamate analogues of morphinan at opioid receptors
Bioorganic & Medicinal Chemistry Letters 2007.0
Design and synthesis of 10-oxo derivative of N-cyclopropylmethyl (−)-6β-acetylthiodihydro-normorphine, a potentially κ-selective opioid receptor ligand
Bioorganic & Medicinal Chemistry Letters 1995.0
2-Aminothiazole-Derived Opioids. Bioisosteric Replacement of Phenols
Journal of Medicinal Chemistry 2004.0
Discovery of a Highly Selective and Potent κ Opioid Receptor Agonist from N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaines with Reduced Central Nervous System (CNS) Side Effects Navigated by the Message–Address Concept
Journal of Medicinal Chemistry 2019.0
Highly selective .kappa.-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted cyclohexyl]arylacetamide derivatives
Journal of Medicinal Chemistry 1990.0
Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology
Bioorganic & Medicinal Chemistry Letters 2008.0
Versatile Picklocks To Access All Opioid Receptors: Tuning the Selectivity and Functional Profile of the Cyclotetrapeptide c[Phe-<scp>d</scp>-Pro-Phe-Trp] (CJ-15,208)
Journal of Medicinal Chemistry 2016.0
Selective .kappa.-Opioid Agonists: Synthesis and Structure-Activity Relationships of Piperidines Incorporating an Oxo-Containing Acyl Group
Journal of Medicinal Chemistry 1994.0