Results 41 to 50 of about 6,519,345 (216)
Ionotropic Glutamate Receptors in Epilepsy: A Review Focusing on AMPA and NMDA Receptors
Biomolecules, 2020 It is widely accepted that glutamate-mediated neuronal hyperexcitation plays a causative role in eliciting seizures. Among glutamate receptors, the roles of N-methyl-D-aspartate (NMDA) and α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA ...
Takahisa Hanada
semanticscholar +1 more source
Structural basis of THC analog activity at the Cannabinoid 1 receptor
Nature CommunicationsTetrahydrocannabinol (THC) is the principal psychoactive compound derived from the cannabis plant Cannabis sativa and approved for emetic conditions, appetite stimulation and sleep apnea relief.
Thor S. Thorsen +15 more
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Frontiers in Neuroscience, 2022 Understanding risk factors for substance use disorders (SUD) can facilitate medication development for SUD treatment. While a rich literature exists discussing environmental factors that influence SUD, fewer articles have focused on genetic factors that ...
Chloe J. Jordan, Zheng-Xiong Xi
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Frontiers in PharmacologyCardiotoxicity and QT interval prolongation have been a common cause of withdrawal of drugs from the market. FCN-437c is an oral, second-generation, potent, and selective CDK4/6 inhibitor for the treatment of patients with HR+/HER2- metastatic breast ...
Lin Zhao +10 more
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A Non-D2-Receptor-Binding Drug for the Treatment of Schizophrenia.
New England Journal of Medicine, 2020 BACKGROUND An oral compound, SEP-363856, that does not act on dopamine D2 receptors but has agonist activity at trace amine-associated receptor 1 (TAAR1) and 5-hydroxytryptamine type 1A (5-HT1A) receptors, may represent a new class of psychotropic agent ...
K. Koblan +6 more
semanticscholar +1 more source
Nuclear Receptors in Drug Metabolism, Drug Response and Drug Interactions.
Nuclear Receptor Research, 2015 Orally delivered small-molecule therapeutics are metabolized in the liver and intestine by phase I and phase II drug-metabolizing enzymes (DMEs), and transport proteins coordinate drug influx (phase 0) and drug/drug-metabolite efflux (phase III).
C. Prakash +6 more
semanticscholar +1 more source
Probing Cortical Sites of Antipsychotic Drug Action with in vivo Receptor Imaging
Behavioural Neurology, 2000 Imaging receptors using radioactive ligands has allowed direct determination of the sites of action of antipsychotic drugs. Initial studies relating antipsychotic drug efficacy to action at striatal dopamine D2-like receptors have recently been ...
P. Shaw, L. S. Pilowsky
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Journal of Pharmacy and Pharmacology, 1966 Abstract The rate of association of drug and receptor when limited by diffusion alone will correspond to a basic rate of 2·5 × 109 litres/mole sec and will have a net activation energy of 3–4 kcal/mole. This rate will not be significantly increased by attractive forces between drug and receptor but could be reduced by repulsive forces ...
openaire +2 more sources
Muscarinic acetylcholine receptors as targets for drug development [PDF]
Medicinski PodmladakMuscarinic acetylcholine receptors (mAChRs) are a subfamily of G protein-coupled receptors that have been identified as promising targets for drug development. Five different mAChR subtypes regulate various fundamental functions.
Stojković Maja +2 more
doaj +1 more source
Journal of Pharmacological Sciences, 2013 Calcium is a ubiquitous intracellular signaling molecule required for initiating and regulating neuronal functions. Ca2+ release from intracellular stores in the endoplasmic reticulum into intracellular spaces via intracellular Ca2+–releasing channels ...
Koji Mizuno +2 more
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