Results 51 to 60 of about 79,681,589 (222)

Effect of the replacement of the o-methoxyphenyl moiety with nitrogen-containing aromatic rings within N-phenyl-piperazine and phenoxy-ethylamine-based 1,3-dioxo/oxathio/dithiolanes as α1 and 5-HT1A receptor ligands

Results in Chemistry, 2022
In the present work, nineteen analogues of 1-[(2,2-Diphenyl-1,3-dioxolan-4-yl)methyl]-4-(2-methoxyphenyl)piperazine 5 and N-[2-(2-Methoxyphenoxy)ethyl]-2,2-diphenyl-1,3-dioxolane-4-methanamine 18 were synthesized.
Claudia Sorbi, Silvia Franchini, Michela Buccioni, Antonio Cilia, Lorenza Pirona, Livio Brasili   +5 more
doaj   +1 more source

Artificial Intelligence‐Driven Natural Product Drug Discovery: From Computational Genome Mining to Clinical Translation

Medicinal Research Reviews, EarlyView.
ABSTRACT Natural products (NPs) have historically yielded numerous therapeutic agents, yet their integration into modern drug discovery has been constrained by chemical complexity, low abundance, laborious dereplication, and limited target annotation.
Antonio Lavecchia
wiley   +1 more source

Changes in functional coupling of 5-HT1A receptor to the G-protein in neocortex temporal tissues of patients with temporal lobe epilepsy

Revista Médica del Hospital General de México, 2018
Background: The 5-hydroxytryptamine-1A receptors are known to be involved in the inhibition of seizures in epilepsy. Objective: The main aim of the present study is to determine the functional coupling to G-protein of the 5-HT1A receptor through 8-OH ...
M. Cuellar-Herrera, L. Rocha, N. Saleh-Subaie, F. Velasco, G. Aguado-Carrillo, M. Alonso-Vanegas, R. Guevara-Guzmán, A.L. Velasco   +7 more
doaj   +1 more source

Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)‐VK4‐116, as a Non‐Opioid Medication for the Treatment of Opioid Use Disorder

Medicinal Research Reviews, EarlyView.
ABSTRACT Opioid use disorder (OUD) remains a major global health challenge, and currently approved treatments (methadone, buprenorphine, and naltrexone) are all opioid receptor‐targeting drugs with limitations in access, adherence, stigma, and use in polysubstance use disorders. Because the dopamine D3 receptor (D3R) is enriched in limbic brain regions
Chia‐Kuei Wu, Yu‐Chih Lin, Junfeng Huang, Bangwei Ding, Pramod Terse, Rahul Nandre, Haksong Jin, Molly Congdon, Kun Shen, Philip Sanderson, Gregory Tawa, Stephanie Mounaud, Marta De Santis, Donald Lo, Elizabeth A. Ottinger, Amy Hauck Newman   +15 more
wiley   +1 more source

The effects of AP521, a novel anxiolytic drug, in three anxiety models and on serotonergic neural transmission in rats

Journal of Pharmacological Sciences, 2015
We investigated the anxiolytic effects and mechanism of action of a new anxiolytic drug, (R)-piperonyl-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridine-3- carboxamide hydrochloride (AP521).
Ken-ichi Kasahara, Shinji Hashimoto, Tsuyoshi Hattori, Koh Kawasaki, Ryuichi Tsujita, Osamu Nakazono, Katsuyuki Takao, Hiromu Kawakubo, Tadashi Nagatani   +8 more
doaj   +1 more source

5‐Methoxy‐N,N‐dimethyltryptamine (5‐MeO‐DMT) for alcohol use disorder: An open‐label, phase 2, proof‐of‐concept, clinical trial

Addiction, EarlyView.
Abstract Background and Aims Psychedelic drugs may help treat alcohol use disorder (AUD). This study evaluated BPL‐003, a novel intranasal powder formulation of 5‐methoxy‐N,N‐dimethyltryptamine (5‐MeO‐DMT) benzoate salt, in people with moderate–severe AUD enrolled in a standard of care, 10‐week programme of relapse‐prevention oriented Cognitive ...
John Marsden, Michael Kelleher, Fiona Dunbar, Anna O. Ermakova, Luke Mitcheson, Claire Roberts, James J. Rucker, Gemma Scott, Ivan Saeger, Francesca Small, Mathieu Seynaeve   +10 more
wiley   +1 more source

The 5-HT1A Receptor Antagonist p-MPPI Blocks Responses Mediated by Postsynaptic and Presynaptic 5-HT1A Receptors

Pharmacology Biochemistry and Behavior, 1997
The present experiments examined the ability of the novel 5-HT1A receptor antagonist to block responses mediated by postsynaptic and presynaptic 5-HT1A receptors in vivo. Pretreatment with p-MPPI reduced or blocked the effect of the 5-HT1A receptor agonist 8-OH-DPAT on two responses mediated by postsynaptic 5-HT1A receptors, reduction of body ...
A R, Allen, A, Singh, Z P, Zhuang, M P, Kung, H F, Kung, I, Lucki   +5 more
openaire   +2 more sources

5-HT1A receptor agonist affects fear conditioning through stimulations of the postsynaptic 5-HT1A receptors in the hippocampus and amygdala [PDF]

European Journal of Pharmacology, 2006
Evidence from preclinical and clinical studies has shown that 5-HT(1A) receptor agonists have anxiolytic actions. The anxiolytic actions of 5-HT(1A) receptor agonists have been tested by our previous studies using fear conditioning. However, little is known about the brain regions of anxiolytic actions of 5-HT(1A) receptor agonists in this paradigm. In
Li, XiaoBai, Inoue, Takeshi, Abekawa, Tomohiro, Weng, ShiMin, Nakagawa, Shin, Izumi, Takeshi, Koyama, Tsukasa   +6 more
openaire   +3 more sources

Ingestão de alimento após a ativação de receptores 5-HT1A do núcleo arqueado do hipotálamo e da área hipotalâmica lateral de ratas em duas fases do ciclo estral [PDF]

, 2009
Tese (doutorado) - Universidade Federal de Santa Catarina, Centro de Ciências Biológicas, Programa de Pós-Graduação em Neurociências, Florianópolis, 2009.O presente estudo examinou os efeitos da injeção local de metergolina (MET, antagonista de ...
Steffens, Sérgio Murilo
core  

Comparative effectiveness, safety and acceptability of pharmacological and psychosocial interventions for the treatment of cannabis use disorder: A network meta‐analysis

Addiction, EarlyView.
Abstract Aim Our primary aim was to conduct a network meta‐analysis (NMA) for the effectiveness, safety and acceptability of all psychosocial interventions and all pharmacotherapies for cannabis use disorder (CUD). Methods We conducted a NMA of studies identified from two completed systematic reviews examining the effectiveness, safety and ...
Monika Halicka, Francesca Spiga, Tom P. Freeman, Suzanne Nielsen, Jelena Savović, Julian P. T. Higgins, Deborah M. Caldwell   +6 more
wiley   +1 more source