“Selective” serotonin 5-HT2A receptor antagonists
Blockade of the serotonin 5-HT 2A G protein-coupled receptor (5-HT 2A R) is a fundamental
pharmacological characteristic of numerous antipsychotic medications, which are FDA …
pharmacological characteristic of numerous antipsychotic medications, which are FDA …
The novel non-hallucinogenic compound DM506 (3-methyl-1, 2, 3, 4, 5, 6-hexahydroazepino [4, 5-b] indole) induces sedative-and anxiolytic-like activity in mice by a …
The anxiolytic and sedative-like effects of 3-methyl-1, 2, 3, 4, 5, 6-hexahydroazepino [4, 5-b]
indole (DM506), a non-hallucinogenic compound derived from ibogamine, were studied in …
indole (DM506), a non-hallucinogenic compound derived from ibogamine, were studied in …
Evaluating pimavanserin tartrate as a treatment in Parkinson's disease
T Müller - Expert Opinion on Pharmacotherapy, 2024 - Taylor & Francis
Introduction Pimavanserin is an efficacious, atypical neuroleptic. It ameliorates the frequency
and severity of hallucinations and delusions in patients with Parkinson's disease with …
and severity of hallucinations and delusions in patients with Parkinson's disease with …
Design, Synthesis, Molecular Docking, and Biological Evaluation of Novel Pimavanserin-Based Analogues as Potential Serotonin 5-HT2A Receptor Inverse Agonists
There is concern for important adverse effects with use of second-generation antipsychotics
in Parkinson's disease psychosis (PDP) and dementia-related psychosis. Pimavanserin is …
in Parkinson's disease psychosis (PDP) and dementia-related psychosis. Pimavanserin is …
Synthesis, docking studies and pharmacological evaluation of serotoninergic ligands containing a 5-norbornene-2-carboxamide nucleus
R Sparaco, E Kędzierska, AA Kaczor, A Bielenica… - Molecules, 2022 - mdpi.com
A new series of 5-norbornene-2-carboxamide derivatives was prepared and their affinities to
the 5-HT1A, 5-HT2A, and 5-HT2C receptors were evaluated and compared to a previously …
the 5-HT1A, 5-HT2A, and 5-HT2C receptors were evaluated and compared to a previously …
Effects of (−)‐MBP, a novel 5‐HT2C agonist and 5‐HT2A/2B antagonist/inverse agonist on brain activity: A phMRI study on awake mice
PK Sathe, GR Ramdasi, K Giammatteo… - Pharmacology …, 2023 - Wiley Online Library
Abstract A novel serotonin ligand (−)‐MBP was developed for the treatment of schizophrenia
that has 5‐HT2A/2B antagonist activity together with 5‐HT2C agonist activity. The multi …
that has 5‐HT2A/2B antagonist activity together with 5‐HT2C agonist activity. The multi …
Development of 2-Aminotetralin-Type Serotonin 5-HT1 Agonists: Molecular Determinants for Selective Binding and Signaling at 5-HT1A, 5-HT1B, 5-HT1D, and 5 …
RP McGlynn, M Cui, B Brems, O Holbrook… - ACS Chemical …, 2023 - ACS Publications
The serotonin (5-hydroxytryptamine, 5-HT) 5-HT1 G-protein coupled receptor subtypes (5-
HT1A/1B/1D/1E/1F) share a high sequence homology, confounding development of subtype …
HT1A/1B/1D/1E/1F) share a high sequence homology, confounding development of subtype …
Conformationally Selective 2-Aminotetralin Ligands Targeting the alpha2A-and alpha2C-Adrenergic Receptors
Many important physiological processes are mediated by alpha2A-and alpha2C-adrenergic
receptors (α2Rs), a subtype of class AG protein-coupled receptors (GPCRs). However, α2R …
receptors (α2Rs), a subtype of class AG protein-coupled receptors (GPCRs). However, α2R …
Synthesis and in vitro evaluation of novel amino-phenylmethylene-imidazolone 5-HT 2A receptor antagonists
GE Dwulet - RSC Medicinal Chemistry, 2024 - pubs.rsc.org
Many drugs target the serotonin 2A (5-HT2A) receptor, including psychedelics,
antidepressants, and antipsychotics. This study investigates the 5-HT2A receptor-binding …
antidepressants, and antipsychotics. This study investigates the 5-HT2A receptor-binding …
Serotonin 5-HT2A, 5-HT2B, and 5-HT2C Receptor Inverse Agonists
R Booth - US Patent App. 18/578,066, 2024 - Google Patents
2024-01-25 Assigned to NATIONAL INSTITUTES OF HEALTH (NIH), US DEPT. OF HEALTH
AND HUMAN SERVICES (DHHS), US GOVERNMENT reassignment NATIONAL …
AND HUMAN SERVICES (DHHS), US GOVERNMENT reassignment NATIONAL …