G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

International Union of Basic and Clinical Pharmacology. CX. Classification of receptors for 5-hydroxytryptamine; pharmacology and function

NM Barnes, GP Ahern, C Becamel, J Bockaert… - Pharmacological …, 2021 - ASPET
5-HT receptors expressed throughout the human body are targets for established
therapeutics and various drugs in development. Their diversity of structure and function …

Bespoke library docking for 5-HT2A receptor agonists with antidepressant activity

AL Kaplan, DN Confair, K Kim, X Barros-Álvarez… - Nature, 2022 - nature.com
There is considerable interest in screening ultralarge chemical libraries for ligand discovery,
both empirically and computationally,,–. Efforts have focused on readily synthesizable …

Identification of 5-HT2A receptor signaling pathways associated with psychedelic potential

J Wallach, AB Cao, MM Calkins, AJ Heim… - Nature …, 2023 - nature.com
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A
receptor activation mediates psychedelic effects, prototypical psychedelics activate both 5 …

Mechanisms and molecular targets surrounding the potential therapeutic effects of psychedelics

AM Jaster, J González-Maeso - Molecular psychiatry, 2023 - nature.com
Psychedelics, also known as classical hallucinogens, have been investigated for decades
due to their potential therapeutic effects in the treatment of neuropsychiatric and substance …

Synaptic and circuit functions of multitransmitter neurons in the mammalian brain

ML Wallace, BL Sabatini - Neuron, 2023 - cell.com
Neurons in the mammalian brain are not limited to releasing a single neurotransmitter but
often release multiple neurotransmitters onto postsynaptic cells. Here, we review recent …

[HTML][HTML] Molecular mechanisms of action of systemic lidocaine in acute and chronic pain: a narrative review

H Hermanns, MW Hollmann, MF Stevens, P Lirk… - British journal of …, 2019 - Elsevier
Systemic administration of the local anaesthetic lidocaine is antinociceptive in both acute
and chronic pain states, especially in acute postoperative and chronic neuropathic pain …

Psychedelics as anti-inflammatory agents

TW Flanagan, CD Nichols - International Review of Psychiatry, 2018 - Taylor & Francis
Abstract Serotonin (5-hydroxytryptamine, 5-HT) 2A receptor agonists have recently emerged
as promising new treatment options for a variety of disorders. The recent success of these …

Cryo-EM structure of the serotonin 5-HT1B receptor coupled to heterotrimeric Go

J García-Nafría, R Nehmé, PC Edwards, CG Tate - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) form the largest family of receptors encoded by the
human genome (around 800 genes). They transduce signals by coupling to a small number …

Central 5-HT receptors and their function; present and future

T Sharp, NM Barnes - Neuropharmacology, 2020 - Elsevier
Since our review of central 5-HT receptors and their function twenty years ago, no new 5-HT
receptor has been discovered and there is little evidence that this situation will change in the …