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Enhanced delayed matching performance in younger and older macaques administered the 5-HT 4 receptor agonist, RS 17017

Autor: Alvin V. Terry, David J. Fontana, William J. Jackson, Jerry J. Buccafusco, Douglas W. Bonhaus, Paul Weller, E.H.F. Wong, Mark A. Prendergast, Richard M. Eglen

Publikováno v: Psychopharmacology. 135:407-415

Recent evidence indicates that the 5-HT4 subtype of serotonin receptor may modulate central cholinergic activity in regions of the mammalian CNS important to memory such as the frontal cortex, hippocampus and amygdala. These receptors could represent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e266112b49bba91707bdb1f42001010e
https://doi.org/10.1007/s002130050529

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[ 3 H]RS 57639, a High Affinity, Selective 5-HT 4 Receptor Partial Agonist, Specifically Labels Guinea-pig Striatal and Rat Cloned (5-HT 4S and 5-HT 4L ) Receptors

Autor: Dana N. Loury, Julius Berger, Sherry A. O. Hsu, E. Leung, Robin D. Clark, E.H.F. Wong, T.A Branchek, N Adham, Richard M. Eglen, Douglas W. Bonhaus

Publikováno v: Neuropharmacology. 36:671-679

RS 57639, by being a partial agonist in rat esophagus but a competitive antagonist in guinea-pig ileum, is one of several ligands which operationally discriminate among 5-HT4 receptors in different tissues. The discovery of splice variants of the 5-H

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e287e21a30cd6cedf8d72e7fac285213
https://doi.org/10.1016/s0028-3908(97)00039-7

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Rs-100235: A high affinity 5-HT4 receptor antagonist

Autor: Richard M. Eglen, E.H.F. Wong, Flippin Lee Allen, L.G. Johnson, Robin D. Clark, Alam Jahangir, Douglas W. Bonhaus, E. Leung, James Langston

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2119-2122

The 1,4-benzodioxanyl ketone 14 (RS-100235) was found to be high affinity 5-HT 4 antagonist with potent in vivo activity and a sustained duration of action in the anesthetized pig.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::84003d258ad37ebdbc52b99665f94d13
https://doi.org/10.1016/0960-894x(95)00358-z

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Synthesis and preliminary pharmacological evaluation of 2-benzyloxy substituted aryl ketones as 5-HT4 receptor antagonists

Autor: Alam Jahangir, A.B. Miller, K.K. Weinhardt, E.H.F. Wong, Douglas W. Bonhaus, Richard M. Eglen, Robin D. Clark, James Langston, E. Leung

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:2481-2484

Structural modification of the 2-methoxy group and at the 4-position of the piperidine ring of the 5-HT4 partial agonist 1 led to analogues with increased affinity for the 5-HT4 receptor and loss of agonist activity. Similar modification of 2 resulte

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::469b2c5caee961383eecb899e230eb0b
https://doi.org/10.1016/s0960-894x(01)80414-5

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Quantitative autoradiography of 5-HT4 receptors in brains of three species using two structurally distinct radioligands, [3H]GR113808 and [3H]BIMU-1

Autor: Douglas W. Bonhaus, Lyn B. Jakeman, Richard M. Eglen, E.H.F. Wong, Z.P. To

Publikováno v: Neuropharmacology. 33:1027-1038

Recent radioligand binding studies have demonstrated the presence of 5-HT 4 receptors throughout the nigrostriatal and mesolimbic systems of mammalian brain. In many regions, the binding has not yet been correlated with functional responses. The pres

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::900eea51c6041122e21eb04be8093819
https://doi.org/10.1016/0028-3908(94)90162-7

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(R) and (S) RS 56532: Mixed 5-HT3 and 5-HT4 receptor ligands with opposing enantiomeric selectivity

Autor: E.H.F. Wong, Richard M. Eglen, Douglas W. Bonhaus, Robin D. Clark, R. L. Whiting, L.G. Johnson, W.L. Smith, C.-H. Lee, E. Leung

Publikováno v: Neuropharmacology. 33:515-526

The pharmacological properties of the (R) and (S) enantiomers of RS 56532 have been studied in vitro and in vivo. In radioligand binding studies at 5-HT4 receptors in guinea-pig striatum, (S) RS 56532 exhibited a higher affinity than (R) RS 56532 (-l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17841ead36a7434ce2ad2043c52aa4c9
https://doi.org/10.1016/0028-3908(94)90083-3

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Comparison of potencies of 5-HT3 receptor antagonists at inhibiting aversive behavior to illumination and the von Bezold-Jarisch reflex in the mouse

Autor: David J. Fontana, E.H.F. Wong, Scott E. Daniels, C.-H. Lee, M. Khabbaz, Richard M. Eglen, T. Kilfoil

Publikováno v: Neuropharmacology. 33:227-234

The inhibitory effects of ondansetron and R and S zacopride on aversive behavior to light and the von Bezold-Jarisch reflex have been compared in mouse. The potencies (ID 50 , μg/kg i.v.) of compounds at inhibiting the von Bezold-Jarisch reflex, eli

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9331c3b041acdee4884c1ef5eb76a4ce
https://doi.org/10.1016/0028-3908(94)90013-2

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N-(quinuclidin-3-YL)-1,8,-naphthalimides with 5-HT3 receptor antagonist and 5-HT4 receptor agonist properties

Autor: Berger Jacob, Richard M. Eglen, E.H.F. Wong, E. Leung, Robin D. Clark, W.L. Smith, C.-H. Lee, K.K. Weinhardt

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:1375-1378

The enantiomers of N -(quinuclidin-3-yl)-4-amino-3-chloro-1,8-naphthalimide ( 3 ) were examined for interactions at 5-HT 3 and 5-HT 4 receptors. ( R )-3 was found to be a potent 5-HT 3 receptor antagonist while ( S )-3 was found to be a 5-HT 4 recept

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ad15e3d26c7b51c767c27ed54b86e8d7
https://doi.org/10.1016/s0960-894x(00)80352-2

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The action of SDZ 205,557 at 5-hydroxytryptamine (5-HT3 and 5-HT4) receptors

Autor: Richard M. Eglen, L.G. Johnson, R. Alvarez, E.H.F. Wong, E. Leung

Publikováno v: British Journal of Pharmacology. 108:376-382

1. The interaction of the novel antagonist, SDZ 205,557 (2-methoxy-4-amino-5-chloro benzoic acid 2-(diethylamino) ethyl ester), at 5-HT3 and 5-HT4 receptors has been assessed in vitro and in vivo. 2. In guinea-pig hippocampus and in the presence of 0

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::829db1f4163803e4dc61acad8f76d7b8
https://doi.org/10.1111/j.1476-5381.1993.tb12812.x

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Characteristics of 5-HT3 binding sites in NG108-15, NCB-20 neuroblastoma cells and rat cerebral cortex using [3H]-quipazine and [3H]-GR65630 binding

Autor: Richard M. Eglen, Dana N. Loury, A. D. Michel, Eric Stefanich, E.H.F. Wong, Roger L. Whiting, Najam A. Sharif

Publikováno v: British Journal of Pharmacology. 102:919-925

1. The biochemical and pharmacological properties of 5-HT3 receptors in homogenates of NG108-15 and NCB-20 neuroblastoma cells and rat cerebral cortex have been ascertained by the use of [3H]-quipazine and [3H]-GR65630 binding. 2. In NG108-15 and NCB

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a65b2be29a29eceafd28eb821b9fdb93
https://doi.org/10.1111/j.1476-5381.1991.tb12277.x

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