62501-70-6Relevant articles and documents
Nelson,Wennerstrom
, p. 921 (1976)
DOPAMINE D2 RECEPTOR LIGANDS
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Page/Page column 150, (2016/07/05)
The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0- arrestin pathway and/or on the cAMP pathway.
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model
Takahashi, Bitoku,Funami, Hideaki,Iwaki, Takehiko,Maruoka, Hiroshi,Shibata, Makoto,Koyama, Makoto,Nagahira, Asako,Kamiide, Yoshiyuki,Kanki, Satomi,Igawa, Yoshiyuki,Muto, Tsuyoshi
, p. 4792 - 4803 (2015/08/03)
A series of 2-alkylamino nicotinamide analogs was prepared as orally active ghrelin receptor (ghrelinR) inverse agonists. Starting from compound 1, oral bioavailability was improved by modifying metabolically unstable sites and reducing molecular weight. Brain-permeable compound 33 and compound 24 with low brain permeability were tested in rat models of obesity; 30 mg/kg of compound 33 suppressed weight gain. PK/PD analysis revealed that the anti-obesity effect of ghrelinR inverse agonists depends on their brain concentrations.