Pharmacological profile of YM348, a novel, potent and orally active 5-HT2C receptor agonist

Genotoxicity of 2-(3-Chlorobenzyloxy)-6-(piperazinyl)pyrazine, a Novel 5-Hydroxytryptamine2c Receptor Agonist for the Treatment of Obesity: Role of Metabolic Activation

“…They also display elevated insulin and leptin levels and impaired glucose utilization (Tecott et al, 1995;Heisler et al, 1998;Nonogaki et al, 1998). Consistent with these observations, 5-HT 2C agonists have been reported to reduce food intake and body weight in animal models (Bickerdike, 2003;Kimura et al, 2004;Vickers and Dourish, 2004;Dunlop et al, 2005). Conversely, 5-HT 2C antagonists such as antipsychotics increase food intake in rodents and cause weight gain in humans (Masand, 2000;von Meyenburg et al, 2003).…”

WAY-163909 [(7bR, 10aR)-1,2,3,4,8,9,10,10a-Octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole], a Novel 5-Hydroxytryptamine 2C Receptor-Selective Agonist with Anorectic Activity

“…Studies using 5-HT antagonists that differ in selectivity among the 5-HT receptor subtypes have provided evidence supporting a role for the 5-HT 2C receptor in the regulation of this mCPP response Curzon, 1988, 1991). More recently described 5-HT 2C agonists such as Ro 60-0175, WAY-161503, VER-3323, PNU-22394, YM348, and WAY-629 have been reported to reduce food intake and body weight in animal models (Martin et al, 1998;Rosenzweig-Lipson et al, 2000;Vickers et al, 2000Vickers et al, , 2003Welmaker et al, 2000;McCall et al, 2001;Bickerdike, 2003;Hayashi et al, 2004;Kimura et al, 2004;Sabb et al, 2004). Conversely, pharmacological agents exhibiting 5-HT 2C antagonist activity such as antipsychotics increase food intake in rodents and cause weight gain in humans (Kennett and Curzon, 1988;Allison et al, 1999;Masand, 2000;Whitaker, 2000).…”

Synthesis, spectral analysis and in vitro microbiological evaluation of novel ethyl 4-(naphthalen-2-yl)-2-oxo-6-arylcyclohex-3-enecarboxylates and 4,5-dihydro-6-(napthalen-2-yl)-4-aryl-2H-indazol-3-ols

“…In recent years there has been a great deal of interest in exploiting more than one proximal functional group for designing novel structures capable of performing a variety of functions. Taking these considerations into account and as part of our research programme aimed at the synthesis of bioactive novel structurally diverse heterocycles [11][12][13][14][15], we report the molecular conjugation of the naphthyl substituted chalcone moiety with two or more active counterparts that has been designed and synthesised with the hope of producing novel ethyl 4-(naphthalen-2-yl)-2-oxo-6-arylcyclohex-3-enecarboxylates (8)(9)(10)(11)(12)(13)(14) an intermediate with three versatile functional groups i.e. ketone, olefin and ester for the synthesis of 4,5-dihydro-6-(naphthalen-2-yl)-4-aryl-2H-indazol-3-ols (15-21), a novel fused indazole derivative and to study their biopotential against clinically isolated bacterial and fungal strains.…”

“…It shows thermogenic and anorectic effects in animal studies [9]. AL-38022A, (S)-1-(8,9-dihydropyrano[2,3-g]indazol-1(7H)-yl)-propan-2-amine (E) is an indazole derivative drug that acts as a potent and selective agonist for the 5-HT 2 family of serotonin receptors.…”