Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT2A Receptors

AR Blaazer, P Smid, CG Kruse - … : Chemistry Enabling Drug …, 2008 - Wiley Online Library
Agonist activation of central 5‐HT2A receptors results in diverse effects, such as
hallucinations and changes of consciousness. Recent findings indicate that activation of the …

Discovery of Benzamide Analogues as a Novel Class of 5‐HT3 Receptor Agonists

CG Jørgensen, B Frølund, J Kehler… - ChemMedChem, 2011 - Wiley Online Library
A 5‐HT3 receptor agonist based on a benzamide scaffold was identified in a screening of a
small commercial compound library, and an elaborate SAR study originating from this hit …

Synthesis and Structure–Activity Relationships of N-Benzyl Phenethylamines as 5-HT2A/2C Agonists

M Hansen, K Phonekeo, JS Paine… - ACS chemical …, 2014 - ACS Publications
N-Benzyl substitution of 5-HT2A receptor agonists of the phenethylamine structural class of
psychedelics (such as 4-bromo-2, 5-dimethoxyphenethylamine, often referred to as 2C-B) …

The therapeutic potential of 5-HT1A receptors: a patent review

E Lacivita, P Di Pilato, P De Giorgio… - Expert opinion on …, 2012 - Taylor & Francis
Introduction: The 5-HT1A receptors are implicated in mood disorders (anxiety, depression),
in cognition, and in modulation of pain. Nearly 30 years of research in this field, there is still …

The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications.

G Poissonnet, JG Parmentier, JA Boutin… - Mini Reviews in …, 2004 - europepmc.org
5-HT (2) receptors mediate a large array of physiological and behavioral functions in
humans via three distinct subtypes: 5-HT (2A), 5-HT (2B) and 5-HT (2C). While selective 5 …

1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT2A Partial Agonists

CS Dowd, K Herrick-Davis, C Egan… - Journal of medicinal …, 2000 - ACS Publications
Phenylalkylamines such as 1-(4-bromo-2, 5-dimethoxyphenyl)-2-aminopropane (DOB; 1a)
and its corresponding iodo derivative DOI (2) are commonly used 5-HT2 serotonin agonists …

trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines:  A New Class of Potent and Selective 5-HT1A Receptor Ligands as Conformationally Constrained …

R Perrone, F Berardi, NA Colabufo… - Journal of medicinal …, 2001 - ACS Publications
The present paper concerns the influence of conformational parameters on the recognition
by rat 5-HT1A receptors of derivatives 4-[3-(5-methoxy-1, 2, 3, 4-tetrahydronaphthalen-1-yl) …

Subtle Differences among 5-HT3AC, 5-HT3AD, and 5-HT3AE Receptors Are Revealed by Partial Agonists

KL Price, Y Hirayama, SCR Lummis - ACS chemical neuroscience, 2017 - ACS Publications
5-HT3 receptors are members of the Cys-loop family of ligand-gated ion channels, and, like
most members of this family, there are multiple subunits that can contribute to functional …

Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5‐HT2A and 5‐HT2C receptors

C Acuña‐Castillo, C Villalobos… - British journal of …, 2002 - Wiley Online Library
The pharmacological profile of a series of (±)‐2, 5‐dimethoxy‐4‐(X)‐phenylisopropylamines
(X= I, Br, NO2, CH3, or H) and corresponding phenylethylamines, was determined in …

5-HT1A receptor, an old target for new therapeutic agents

E Lacivita, M Leopoldo, F Berardi… - Current Topics in …, 2008 - ingentaconnect.com
The serotonin receptor subtype 5-HT1A was one of the first serotonin receptor subtypes
pharmacologically characterized. Over the last twenty years the 5-HT1A receptor has been …