146715-07-3Relevant articles and documents
Solid-phase radiosynthesis of [11C]WAY 100635
Wilson, Alan A.,DaSilva, Jean N.,Houle, Sylvain
, p. 149 - 154 (1996)
An efficient, fast and simple method is described for the radiosynthesis of the potent and selective 5-HT1A antagonist [O-methyl- 11C]-N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexane carboxamide ([11C]WAY 100635). [11C]Iodomethane was effectively trapped on a C18 reverse-phase cartridge at ambient temperature where it reacted rapidly with the normethyl precursor, N-[2-[4-(2-hydroxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexane carboxamide. Following high performance liquid chromatography purification and formulation, [11C]WAY 100635 was obtained in high radiochemical yields (40%, uncorrected from [11C]Iiodomethane) in a synthesis time of 25 min with an average specific actvity of (at end-of-synthesis) 33 GBq/μmole (900 mCi/μmole).
Synthesis and in vitro and in vivo functional studies of Ortho- substituted phenylpiperazine and N-substituted 4-N-(o- methoxyphenyl)aminopiperidine analogues of WAY100635
Mensonides-Harsema, Marguérite M.,Liao, Yi,B?ttcher, Henning,Bartoszyk, Gerd D.,Greiner, Hartmunt E.,Harting, Jürgen,De Boer, Peter,Wikstr?m, H?kan V.
, p. 432 - 439 (2007/10/03)
WAY100635 (2), N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2- pyridinyl)cyclohexane-carboxamide, is a silent serotonin 5-HT(1A) antagonist, which is now widely used to study the 5-HT(1A) receptor both in vivo and in vitro. In this paper, we describe
N-((phenyl, benzodioxinyl or N-heteroarylpiperazinyl)alkyl)-N-(N-heteroaryl)substituted carboxamides
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, (2008/06/13)
Piperazine derivatives of formula I and their pharmaceutically acceptable acid addition salts are 5-HT1A binding agents, particularly 5-HT1A antagonists and may be used, for example, as anxiolytics. In the formula A is C2-4 alkylene chain optionally substituted by lower alkyl, Z is oxygen or sulphur, R is hydrogen or lower alkyl, R1 is a mono or bicyclic aryl or heteroaryl radical, R2 is a mono or bicyclic heteroaryl radical and R3 is hydrogen or a specified radical such as lower alkyl, cycloalkyl, aryl, heteroaryl or optionally substituted amino.
Pre-clinical Development of a Radioligand for Studies of Central 5-HT1A Receptors in Vivo - [11C]WAY-100635
Pike, Victor W.,McCarron, Julie A.,Hume, Susan P.,Ashworth, Sharon,Opacka-Juffry, Jolanta,et al.
, p. 208 - 227 (2007/10/03)
Syntheses of N-(2-(1-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl))-N-(2-pyridyl)-cyclohexanecarboxamide (WAY-100635) and its desmethyl and descyclohexylcarbonyl analogues are described. WAY-100635 has properties that favour its development as a radioligand f