Discovery and biological characterization of capromorelin analogues with extended half-lives

Ghrelin Gene Products and the Regulation of Food Intake and Gut Motility

“…4). In addition, intrathecal application of CP-464709-18 (Carpino et al, 2002;Atcha et al, 2009), a synthetic GHS-R1a agonist, at L6-S1, but not application at pontomedullary levels or to the thoracic spinal cord, elicited propulsive contractions. The stimulation evoked by intravenous CP-464709-18 was prevented if the pelvic nerve outflows were severed, but not if the spinal cord was cut rostral to the defecation center at L6 -S3, and was also blocked by hexamethonium (Shimizu et al, 2006).…”

Cognitive enhancing effects of ghrelin receptor agonists

“…This has been driven primarily by the hypothesis that agents that mimic the actions of ghrelin may have utility not only in growth hormone replacement therapy but also in disorders requiring increased nutritional intake, such as cancer-induced cachexia, post-operative ileus and potentially in gastrointestinal motility disorders such as neurogenic and diabetic gastroparesis (Binn et al 2006;Murray et al 2005). The medicinal chemistry efforts conducted by a number of pharmaceutical companies led to the identification of relatively high molecular weight and complex structured molecules, such as CP-424391-18 (Pan et al 2001), CP-464709-18 (Carpino et al 2002) and MK-0677 (Patchett et al 1995).…”

Reactions of N-alkylhydrazones of aliphatic ketones

“…Разом з тим відомі декілька прикладів стабільних алкілгідразонів, які циклі-зуються в кислих умовах [50,51] …”