Synthesis of 4,4′-Disubstituted and Spiro-tetrahydroquinolines via Photochemical Cyclization of Acrylanilides and the First Synthesis of (±)-trans-Vabicaserin

Autor: Andreas Haupt, Hannes Koolman, Wilfried Braje

Publikováno v: Synlett. 27:2561-2566

The synthesis of vabicaserin analogues bearing a quaternary center or spiro substitution at the 4-position has been studied via a [6π]-acrylanilide cyclization employing flow photochemistry in a mesoscale and microfluidic flow photoreactor. The meth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c3ecb9863e673c28f2f77a2f21784fa2
https://doi.org/10.1055/s-0035-1562621

A short history of the 5-HT2C receptor: from the choroid plexus to depression, obesity and addiction treatment

Autor: Danniel Hoyer, Angel Pazos, José Palacios

Publikováno v: Psychopharmacology (Berl). 2017 May;234(9-10):1395-1418
Digital.CSIC. Repositorio Institucional del CSIC
instname
UCrea Repositorio Abierto de la Universidad de Cantabria
Universidad de Cantabria (UC)

This paper is a personal account on the discovery and characterization of the 5-HT receptor (first known as the 5-HT receptor) over 30 years ago and how it translated into a number of unsuspected features for a G protein-coupled receptor (GPCR) and a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed8084596ca44e90c19a2f3823357b2d
http://hdl.handle.net/10902/13422

A 6-week randomized, double-blind, placebo-controlled, comparator referenced trial of vabicaserin in acute schizophrenia

Autor: Michael J. Detke, Sharon Rosenzweig-Lipson, Janet B. W. Williams, Earl L. Giller, John M. Kane, Joan H.Q. Shen, Danielle Popp, Yonggang Zhao

Publikováno v: Journal of Psychiatric Research. 53:14-22

Vabicaserin, a potent 5-HT2C receptor agonist, decreases nucleus accumbens extracellular dopamine levels in rats, without affecting striatal dopamine, indicating mesolimbic selectivity. This is the first study of efficacy, safety and tolerability of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bde4ea53e002c5370eab45d0b731ff91
https://doi.org/10.1016/j.jpsychires.2014.02.012

Systemic administration of 5-HT2C receptor agonists attenuates muscular hyperalgesia in reserpine-induced myalgia model

Autor: Mina Tsukamoto, Tomoya Oe, Yukinori Nagakura, Tomonari Watabiki, Yasuaki Shimizu, Hiroyuki Ito, Shin-Ichi Ogino, Tohru Ozawa

Publikováno v: Pharmacology Biochemistry and Behavior. 108:8-15

Fibromyalgia is a prevalent musculoskeletal disorder characterized by chronic widespread pain that significantly reduces quality of life in patients. Due to the lack of consistently effective treatment, the development of improved therapies for treat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f18c0dad3a3b32268e318a90e8acb336
https://doi.org/10.1016/j.pbb.2013.04.007

Characterization of Vabicaserin (SCA-136), a Selective 5-Hydroxytryptamine 2C Receptor Agonist

Autor: John Dunlop, Gary Stack, Menelas N. Pangalos, Joseph Coupet, Deborah L. Smith, Sharon Rosenzweig-Lipson, James E. Barrett, Hossein Mazandarani, Boyd Harrison, Jean Zhang, Siva Ramamoorthy, Lee E. Schechter, Guoming Zhang, Stephanie W. Watts, Stanley Nawoschik

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 337:673-680

The 5-hydroxytryptamine 2C (5-HT 2C ) receptor subtype has received considerable attention as a target for drug discovery, having been implicated in a wide variety of disorders. Here, we describe the in vitro pharmacological profile of the novel 5-HT

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be883274f8e998bcc136daf48f9bd677
https://doi.org/10.1124/jpet.111.179572