- Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors
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The selectivity for 5-HT1A versus D4 receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tet
- Mangin, Floriane,Dilly, Sebastien,Joly, Benoit,Scuvee-Moreau, Jacqueline,Evans, Jon,Setola, Vincent,Roth, Bryan L.,Liegeois, Jean-Francois
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supporting information; experimental part
p. 4550 - 4554
(2012/08/08)
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- Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers
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Molecular imprinting produces network polymers with recognition sites for imprint molecules. The high binding affinity and selectivity in conjunction with the polymers' physical robustness positions molecular imprinted polymers (MIPs) as candidates for us
- O'Connor, Naphtali A.,Paisner, David A.,Huryn, Donna,Shea, Kenneth J.
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p. 1680 - 1689
(2007/10/03)
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- USE OF 5-HT 1A? RECEPTOR ANTAGONISTS FOR THE TREATMENT OF URINARY INCONTINENCE
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Compounds which: (a) bind to a 5-HT1A receptor with an affinity of at least 10M, (b) bind to a 5-HT1A receptor with an affinity at least 50-fold stronger than the affinity with which the compound binds to an alpha 1-adrenergic receptor, and (c) exhibi
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- USE OF 5-HT1A RECEPTOR ANTAGONISTS FOR THE TREATMENT OF URINARY INCONTINENCE
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The present invention discloses compositions and methods for treating neuromuscular dysfunction of the lower urinary tract in mammals, including humans, using serotonin 5-HT 1A receptor antagonist compounds that exert their inhibitory effects via pre-syna
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- Treatment of cognitive disorders with piperazine derivatives
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Piperazine derivatives of formula (I) are useful in the treatment of cognitive disorders. In formula (I), X is a group of (IIa): --(CH2)n CR2 R3 CONR4 R5 or (IIIb): --A--NR6 COR7 where n, A, R, R1, R2, R3, R4, R5, R6 and R7 have specified meanings. STR1
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- Pre-clinical Development of a Radioligand for Studies of Central 5-HT1A Receptors in Vivo - [11C]WAY-100635
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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
- Pike, Victor W.,McCarron, Julie A.,Hume, Susan P.,Ashworth, Sharon,Opacka-Juffry, Jolanta,et al.
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p. 208 - 227
(2007/10/03)
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