Molecular Pharmacology
2026
Lindsay P. Cameron, Alaina M Jaster, Raul A Ramos et al.
3 citations
2,5-dimethoxy-4-iodoamphetamine (DOI) is a phenethylamine psychedelic with high affinity for 5-HT2 receptors. In 2022 and 2023, the US Drug Enforcement Administration proposed to place DOI, along with a similar compound, 2,5-dimethoxy-4-chloroamphetamine, in Schedule I of the Controlled Substances Act based on their psychoactivity and alleged abuse potential. Here, we describe the history of...
Molecular Pharmacology
October 17, 2024
Ivone Gomes, Achla Gupta, Elyssa B Margolis et al.
21 citations
Ketamine is a glutamate receptor antagonist that was developed over 50 years ago as an anesthetic agent. At subanesthetic doses, ketamine and some metabolites are analgesics and fast-acting antidepressants, presumably through targets other than glutamate receptors. We tested ketamine and its metabolites for activity as allosteric modulators of opioid receptors expressed as recombinant receptors...
Molecular Pharmacology
August 16, 2024
Armida Miranda-Riestra, Montserrat G Cercós, Citlali Trueta et al.
4 citations
Melatonin (N-acetyl-5-methoxytryptamine) is an indoleamine secreted by the pineal gland during the dark phase of the photoperiod. Its main function is the synchronization of different body rhythms with the dark-light cycle. Research on melatonin has significantly advanced since its discovery and we now know that it has considerable significance in various physiological processes, including...
Molecular Pharmacology
2003
Barbara J. Ebersole, Irache Visiers, Harel Weinstein et al.
72 citations
Based on experiment and computational simulation, we present a structural explanation for the differing efficacies of indole agonists at the human serotonin 5-HT2A receptor (5HT2AR). We find that serotonin [5-hydroxytryptamine (5-HT)] forms hydrogen-bonds with Ser3.36 in helix 3 and Ser5.46 in helix 5. Disruption of these hydrogen bonds by methyl-substitution of the cationic primary amine or of...
Molecular Pharmacology
December 1, 2001
James R. Bunzow, Mark S. Sonders, Seksiri Arttamangkul et al.
644 citations
The trace amine para-tyramine is structurally and functionally related to the amphetamines and the biogenic amine neurotransmitters. It is currently thought that the biological activities elicited by trace amines such as p-tyramine and the psychostimulant amphetamines are manifestations of their ability to inhibit the clearance of extracellular transmitter and/or stimulate the efflux of...
Molecular Pharmacology
1997
B Badio, W L Padgett, J W Daly
52 citations
Ibogaine noncompetitively blocked (IC50 approximately 20 nM) 22NaCl influx through ganglionic-type nicotinic receptor channels of rat pheochromocytoma PC12 cells. The major metabolite O-des-methylibogaine was 75-fold less active, and O-t-butyl-O-des-methylibogaine was 20-fold less active. Ibogaine was relatively weak as a blocker (IC50 approximately 2000 nM) of the neuromuscular-type nicotinic...
Molecular Pharmacology
November 1, 1990
T. Branchek, N. Adham, M. Macchi et al.
77 citations
The binding properties of the 5-hydroxytryptamine2 (5-HT2) receptor have been the subject of much interest and debate in recent years. The hallucinogenic amphetamine derivative 4-bromo-2,5-dimethoxyphenylisopropylamine (DOB) has been shown to bind to a small number of binding sites with properties very similar to [3H]ketanserin-labeled 5-HT2 receptors, but with much higher agonist affinities....
Molecular Pharmacology
February 1, 1987
R. A. Lyon, K. Davis, M. Titeler
106 citations
3H-(+/-)-4-Bromo-2,5-dimethoxyphenylisopropylamine (3H-DOB), a putative agonist radioligand, was synthesized and used to label 5-HT2 receptors in a particulate fraction prepared from rat frontal cortex tissue homogenates. The specific binding (defined by the difference in 3H-DOB binding in the presence and absence of 10(-6) M cinanserin, a potent and specific 5-HT2 antagonist) displayed high...
Molecular Pharmacology
July 1, 1976
Richard A. Lovell, Daniel X. Freedman
54 citations
A method in vitro designed to determine specifically the stereospecificity of tissue receptor sites was used to study the characteristics of d-lysergic acid diethylamide (LSD) binding by rat brain particulates and the effects of selectively chosen drugs. There is a high- and a low-affinity binding, and both are stereospecific. The high-affinity binding is saturable (half-saturation at 4 nM) and...