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[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor
TLDR
Autoradiographic studies in rhesus monkey brain showed that [18F]MK-9470 binding is aligned with the reported distribution of CB1 receptors with high specific binding in the cerebral cortex, cerebellum, caudate/putamen, globus pallidus, substantia nigra, and hippocampus, and PET imaging studies in human research subject demonstrated behavior very similar to that seen in monkeys. Expand
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
TLDR
Diverse lines of evidence, including genetic and pharmacological data obtained in rodents and humans, support a role for the melanocortin MC(3) and MC(4) receptors in the regulation of energy homeostasis. Expand
Antiobesity Efficacy of a Novel Cannabinoid-1 Receptor Inverse Agonist, N-[(1S,2S)-3-(4-Chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide
TLDR
It is demonstrated that MK-0364 is a highly potent and selective CB1R inverse agonist and that it is orally active in rodent models of obesity. Expand
Identification of Phe313 of the gonadotropin-releasing hormone (GnRH) receptor as a site critical for the binding of nonpeptide GnRH antagonists.
TLDR
Results show that Phe313 of the GnRH receptor is critical for the binding of this structural class of GnRH antagonists and that the dog receptor can be "humanized" by substituting Leu for Phe. Expand
Structure-Activity Relations of Successful Pharmacologic Chaperones for Rescue of Naturally Occurring and Manufactured Mutants of the Gonadotropin-Releasing Hormone Receptor
TLDR
The ability of different GnRH peptidomimetics to rescue defective GnRHR mutants was a reasonable predictor of the ability to rescue others, even across species lines, although particular mutants could not be rescued by any of the drugs tested. Expand
Molecular mechanism of action of pharmacoperone rescue of misrouted GPCR mutants: the GnRH receptor.
TLDR
This model was used to reveal important pharmacophoric features, and then identify a novel chemical ligand, which was able to rescue a D(98) mutant of the hGnRHR that could not be rescued as effectively by previously known pharmacoperones. Expand
Structure-dependent Impairment of Intracellular Apolipoprotein E4 Trafficking and Its Detrimental Effects Are Rescued by Small-molecule Structure Correctors*
TLDR
It is reported that the intracellular trafficking of apoE4 is impaired in Neuro-2a cells and primary neurons, as shown by measuring fluorescence recovery after photobleaching and disrupting domain interaction with the small-molecule structure correctors GIND25 and PH002. Expand
Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.
TLDR
Substantial improvements in potency were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chloro-substitution of the 1 H-quinolone core. Expand
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.
TLDR
A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary amides. Expand
Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus.
TLDR
A pyridine side-chain terminus has been incorporated into the indole-5-carboxamide and indole -5-acetamide series of GnRH antagonists, and certain branched or cyclic tertiary amides were identified as preferred in each series. Expand
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