Pharmacological activities of optically pure enantiomers of the κ opioid agonist, U50,488, and its cis diastereomer: evidence for three κ receptor subtypes
References (30)
- et al.
Synthesis and absolute configuration of optically pure enantiomers of a kappa opioid receptor agonist
FEBS Lett.
(1987) - et al.
Beneficial effects of the kappa opioid receptor agonist U-50488H in experimental acute brain and spinal cord injury
Brain Res.
(1987) - et al.
[3H]U-69,593, a highly selective ligand for the opioid κ receptor
European J. Pharmacol.
(1985) - et al.
Protein measurement with the Folin phenol reagent
J. Biol. Chem.
(1951) - et al.
Autoradiography of [3H]U-69593 binding sites in rat brain: Evidence for κ opioid receptor subtypes
European J. Pharmacol.
(1988) - et al.
[3H]U-69593 labels a subtype of kappa opiate receptor with characteristics different from that labeled by [3H]ethylketocyclazocine
Life Sci.
(1988) - et al.
Differential antagonism of mu agonists by U50488 H in the rat
Life Sci.
(1987) - et al.
Preparation of rat brain membranes highly enriched with opiate kappa binding sites using site-directed alkylating agents: optimization of binding conditions
Neuropeptides
(1985) - et al.
LY164929:a highly selective ligand for the lower affinity [3H]D-ala2D-Leu5-enkephalin binding site
Neuropeptides
(1988) - et al.
A brief study of the selectivity of norbinaltorphimine, (−)-cycloFOXY, and (+)-cycloFOXY among opioid receptor subtypes in vitro
Neuropeptides
(1988)
Tritiated-6-beta-fluoro-6-desoxy-oxymorphone([3H]FOXY): a new ligand and photoaffinity probe for the μ opioid receptors
Neuropeptides
Stereochemistry: a source of problems in medicinal chemistry
Med. Res. Rev.
Stereochemistry in the analysis of drug-action. Part II
Med. Res. Rev.
A procedure for the rapid evaluation of the discriminative stimulus effects of drugs
J. Pharmacol. Meth.
Cited by (48)
Interactive effects of (±)-trans-U50488 and its stereoisomers with cannabinoids
2021, Pharmacology Biochemistry and BehaviorCitation Excerpt :Most studies investigating U-50488 have used the racemate, often because of the lack of knowledge regarding its enantiomers or their capacity for producing different effects (Ariens, 1987). For example, the enantiomers of (±)-U-50488 have different effects in drug discrimination and antinociception procedures as well as in vivo binding studies (DeCosta et al., 1987; Rothman et al., 1989). In our discrimination studies, (−)-U-50488 produced effects on (±)-U-50488-lever responding and response rate that were more potent than, or similar to, the racemate, respectively; whereas (+)-U-50488 did not increase (±)-U-50488-lever responding or decrease response rate up to doses of 32 mg/kg.
Receptors: Opioid receptors
2021, Encyclopedia of Biological Chemistry: Third EditionBifunctional opioid receptor ligands as novel analgesics
2019, NeuropharmacologyCitation Excerpt :In contrast to μ- and δOP receptors, κOP receptors are largely expressed on presynaptic dopaminergic membranes and inhibit presynaptic neurotransmitter release on activation. Three κOP receptor variants have been characterized (κ1-3OP receptors), though only one (κ1OP receptor) has been cloned (Rothman et al., 1989; Mansson et al., 1994). The κOP receptors are broadly expressed throughout the CNS, including the mesolimbic system, hypothalamus, amygdala, spinal cord, and hypothalamic-pituitary axis (Mansour et al., 1995; Peng et al., 2012; Butelman and Kreek, 2015).
Evidence for multiple mechanisms of kappa opioid tolerance in mesencephalic cultures
2003, Brain ResearchCitation Excerpt :This eliminates variability due to differences in cell numbers between wells. U69,593 is a synthetic, potent opioid that selectively activates kappa opioid receptors [12]. In our previous work, U69,593 showed dose–response inhibition of K+-stimulated dopamine release [5].
Opioid antagonist profile of SC nor-binaltorphimine in the formalin paw assay
1996, Pharmacology Biochemistry and BehaviorDistribution of κ opioid receptor mRNA in adult mouse brain: An in situ hybridization histochemistry study
1994, Molecular and Cellular Neurosciences