The promises and perils of psychedelic pharmacology for psychiatry

TD McClure-Begley, BL Roth - Nature Reviews Drug Discovery, 2022 - nature.com
Psychedelic drugs including psilocybin, N, N ʹ-dimethyltryptamine (DMT) and lysergic acid
diethylamide (LSD) are undergoing a renaissance as potentially useful drugs for various …

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 - Elsevier
HT receptors expressed throughout the human body are targets for established therapeutics
and various drugs in development. Their diversity of structure and function reflects the …

Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD

C Cao, X Barros-Álvarez, S Zhang, K Kim, MA Dämgen… - Neuron, 2022 - cell.com
Summary Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential
targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs. Although the …

A non-hallucinogenic LSD analog with therapeutic potential for mood disorders

V Lewis, EM Bonniwell, JK Lanham, A Ghaffari… - Cell reports, 2023 - cell.com
Hallucinations limit widespread therapeutic use of psychedelics as rapidly acting
antidepressants. Here we profiled the non-hallucinogenic lysergic acid diethylamide (LSD) …

Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants

W Duan, D Cao, S Wang, J Cheng - Chemical Reviews, 2023 - ACS Publications
Psychedelics make up a group of psychoactive compounds that induce hallucinogenic
effects by activating the serotonin 2A receptor (5-HT2AR). Clinical trials have demonstrated …

Structure–activity relationships for psilocybin, baeocystin, aeruginascin, and related analogues to produce pharmacological effects in mice

GC Glatfelter, E Pottie, JS Partilla… - ACS Pharmacology & …, 2022 - ACS Publications
4-Phosphoryloxy-N, N-dimethyltryptamine (psilocybin) is a naturally occurring tertiary amine
found in many mushroom species. Psilocybin is a prodrug for 4-hydroxy-N, N …

Teaching old receptors new tricks: biasing seven-transmembrane receptors

S Rajagopal, K Rajagopal, RJ Lefkowitz - Nature reviews Drug …, 2010 - nature.com
Abstract Seven-transmembrane receptors (7TMRs; also known as G protein-coupled
receptors) are the largest class of receptors in the human genome and are common targets …

Molecular basis of opioid receptor signaling

T Che, BL Roth - Cell, 2023 - cell.com
Opioids are used for pain management despite the side effects that contribute to the opioid
crisis. The pursuit of non-addictive opioid analgesics remains unattained due to the …

LSD-stimulated behaviors in mice require β-arrestin 2 but not β-arrestin 1

RM Rodriguiz, V Nadkarni, CR Means, VM Pogorelov… - Scientific reports, 2021 - nature.com
Recent evidence suggests that psychedelic drugs can exert beneficial effects on anxiety,
depression, and ethanol and nicotine abuse in humans. However, their hallucinogenic side …

Psychedelics as transformative therapeutics

BL Roth, RH Gumpper - American Journal of Psychiatry, 2023 - Am Psychiatric Assoc
Over the past decade, psychedelic compounds have emerged as potentially transformative
therapeutics for a variety of intractable neuropsychiatric conditions. However, historically …