Activity of Parthenolide at 5HT2A Receptors

JT Weber, MF O'Connor, K Hayataka… - Journal of natural …, 1997 - ACS Publications
Parthenolide displaces [3H] ketanserin from 5HT2A receptors from rat and rabbit brain and
cloned 5HT2A receptors. K i's are in the 100− 250 μM range. These results suggest that …

Inverse agonist activity of sarpogrelate, a selective 5-HT2A-receptor antagonist, at the constitutively active human 5-HT2A receptor

HA Muntasir, MA Bhuiyan, M Ishiguro, M Ozaki… - Journal of …, 2006 - Elsevier
Mutations producing constitutively active G-protein coupled receptors have been found in
the pathophysiology of several diseases, implying that inverse agonists at the constitutively …

Assessment of affinity and dissociation ability of a newly synthesized 5-HT2 antagonist, AT-1015: comparison with other 5-HT2 antagonists

M Rashid, M Watanabe, M Nakazawa… - The Japanese Journal …, 2001 - jstage.jst.go.jp
This study investigated the binding affinities of a newly synthesized 5-HT2 antagonist, AT-
1015 (N-[2-[4-(5H-dibenzo [a, d] cyclohepten-5-ylidene)-piperidino] ethyl]-1-formyl-4 …

Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors

S Madapa, WW Harding - Journal of Natural Products, 2015 - ACS Publications
N-Methyllaurotetanine (1) has been reported to display good affinity for the 5-HT1A receptor,
but no structure–affinity studies have been performed to date. The commercially available …

The 5-HT1Dreceptor antagonist GR 127,935 is an agonist at cloned human 5-HT1Dα receptor sites

PJ Pauwels, FC Colpaert - Neuropharmacology, 1995 - Elsevier
The cAMP response of the 5-HT1D receptor antagonist GR 127,935 was compared with 5-
CT and ketanserin at cloned human 5-HT1Dα receptor sites in transfected C6-glial cells. GR …

Selective antagonism of human 5-HT1D and 5-HT1B receptor-mediated responses in stably transfected C6-glial cells by ketanserin and GR 127,935

PJ Pauwels, FC Colpaert - European journal of pharmacology, 1996 - Elsevier
The antagonist effects of ketanserin and 2′-methyl-4′-(5-methyl-1, 2, 4) oxadiazol-3-yl)-
biphenyl-[4-carboxylic acid 4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]-amide (GR …

Binding of Tetrahydrocarboline Derivatives at Human 5-HT5A Receptors

N Khorana, C Smith, K Herrick-Davis… - Journal of medicinal …, 2003 - ACS Publications
On the basis of an earlier finding that 5-methyl-5 H-1, 2, 3, 4-tetrahydropyrido [4, 3-b] indole
(5-methyl-1, 2, 3, 4-tetrahydro-γ-carboline; 1) binds at murine 5-HT5A receptors, preliminary …

DAU 6285: a novel antagonist at the putative 5-HT4 receptor

A Schiavone, E Giraldo, L Giudici, M Turconi… - Life sciences, 1992 - Elsevier
The antagonistic properties of DAU 6285, an azabicycloalkyl benzimidazolone derivative, at
putative 5-hydroxytryptamine 4 (5-HT 4) receptors were investigated in in vitro preparations …

Receptor specificity of the 5HT2 receptor antagonist, LY53857

ML Cohen, W Colbert… - Drug development …, 1985 - Wiley Online Library
LY53857 is a potent antagonist at vascular 5HT2 receptors that lacks prominent α1 or
dopamine antagonist activity. The present report investigates the interaction of LY53857 with …

The 5‐HT4 receptor agonist, tegaserod, is a potent 5‐HT2B receptor antagonist in vitro and in vivo

DT Beattie, JAM Smith, D Marquess… - British journal of …, 2004 - Wiley Online Library
Tegaserod (Zelnorm®) is a potent 5‐hydroxytryptamine4 (5‐HT4) receptor agonist with
clinical efficacy in disorders associated with reduced gastrointestinal motility and transit. The …