A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties

scientific article

A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1016/J.BMCL.2009.02.126
P698PubMed publication ID19307114

P2093author name stringAshley Parker
Neil Moss
Heather Tye
Younggi Choi
Adam Flegg
Spencer Napier
Mark Whitaker
J Thomas Peterson
Derek Cogan
Donna Skow
Christopher Sarko
Andreas Kahrs
Josh Tomlinson
Orietta Meyn
Philip Ramsden
Pui Loke
Raj Nagaraja
P2860cites workRS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonistQ24672108
Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonistQ24672386
5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitroQ24673230
Ablation of serotonin 5-HT(2B) receptors in mice leads to abnormal cardiac structure and functionQ28202523
Involvement of the serotonin 5-HT2B receptor in cardiac hypertrophy linked to sympathetic stimulation: control of interleukin-6, interleukin-1beta, and tumor necrosis factor-alpha cytokine production by ventricular fibroblastsQ28276340
Serotonin 5-HT(2B) receptor blockade prevents reactive oxygen species-induced cardiac hypertrophy in miceQ28285608
Mechanical stress enhances serotonin 2B receptor modulating brain natriuretic peptide through nuclear factor-kappaB in cardiomyocytesQ34564767
Functions of serotonin in hypoxic pulmonary vascular remodelingQ34653768
The importance of plasma protein binding in drug discoveryQ43851506
Neurogenic dural protein extravasation induced by meta-chlorophenylpiperazine (mCPP) involves nitric oxide and 5-HT2B receptor activationQ44326286
Overexpression of the serotonin 5-HT2B receptor in heart leads to abnormal mitochondrial function and cardiac hypertrophyQ44480703
A simple method for predicting serum protein binding of compounds from IC(50) shift analysis for in vitro assaysQ47775437
Altered expression of a limited number of genes contributes to cardiac decompensation during chronic ventricular tachypacing in dogs.Q54567679
The Emergence of Selective 5-HT2B Antagonists Structures, Activities and Potential Therapeutic Applications [General Reviews]Q56551617
Plasma protein binding affinity and its relationship to molecular structure: an in-silico analysisQ79481932
P433issue8
P407language of work or nameEnglishQ1860
P921main subject5-hydroxytryptamine receptor 2BQ4639596
pharmacokineticsQ323936
drug bindingQ14819373
P304page(s)2206-10
P577publication date2009-04-15
P1433published inBioorganic & Medicinal Chemistry LettersQ2709483
P1476titleA new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties
P478volume19

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cites work (P2860)
Q85090837Exploration of the binding of benzimidazole-biphenyl derivatives to hemoglobin using docking and molecular dynamics simulation
Q64951410Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands.
Q34659424Lorcaserin and adiposopathy: 5-HT2c agonism as a treatment for 'sick fat' and metabolic disease
Q48172109Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2C Serotonin Receptor Antagonists
Q82676939The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

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