Results 51 to 60 of about 32,658 (245)

CB2R agonist prevents nicotine induced lung fibrosis

Experimental Lung Research, 2018
Nicotine stimulates fibroblast proliferation while increasing inflammation and fibrosis of tissues. The cannabinoid receptor 1 (CB1R) is mainly located in the CNS, while cannabinoid receptor 2 (CB2R) is located in the immune cells within the body. CB2R regulates inflammatory processes and fibroblast function.We investigated the impact of CB2R agonist ...
Ewelina, Wawryk-Gawda, Katarzyna, Chłapek, Michał K, Zarobkiewicz, Marta, Lis-Sochocka, Patrycja, Chylińska-Wrzos, Anna, Boguszewska-Czubara, Mirosław A, Sławiński, Anna, Franczak, Barbara, Jodłowska-Jędrych, Grażyna, Biała   +9 more
openaire   +3 more sources

Activation of muscle nicotinic acetylcholine receptor channels by nicotinic and muscarinic agonists [PDF]

British Journal of Pharmacology, 1999
The dose‐response parameters of recombinant mouse adult neuromuscular acetylcholine receptor channels (nAChR) activated by carbamylcholine, nicotine, muscarine and oxotremorine were measured. Rate constants for agonist association and dissociation, and channel opening and closing, were estimated from single‐channel kinetic analysis.
G, Akk, A, Auerbach
openaire   +2 more sources

Rates and Equilibria for a Photoisomerizable Antagonist at the Acetylcholine Receptor of Electrophorus Electroplaques [PDF]

, 1985
Voltage-jump and light-flash experiments have been performed on isolated Electrophorus electroplaques exposed simultaneously to nicotinic agonists and to the photoisomerizable compound 2,2'-bis-[α-(trimethylammonium)methyl]-azobenzene (2BQ).
Erlanger, Bernard F., Krouse, Mauri E., Lester, Henry A., Wassermann, Norbert H.   +3 more
core   +1 more source

Differential Contribution of Subunit Interfaces to α 9 α 10 Nicotinic Acetylcholine Receptor Function [PDF]

, 2017
Nicotinic acetylcholine receptors can be assembled from either homomeric or heteromeric pentameric subunit combinations. At the interface of the extracellular domains of adjacent subunits lies the acetylcholine binding site, composed of a principal ...
Boffi, Juan Carlos, Bouzat, Cecilia Beatriz, Collins, Toby, Corradi, Jeremias, Craig, Patricio Oliver, Elgoyhen, Ana Belen, Gill Thind, JasKiran K., Lipovsek, Maria Marcela, Marcovich, Irina, Millar, Neil S., Moglie, Marcelo Javier, Plazas, Paola Viviana   +11 more
core   +3 more sources

Clinical pharmacology and prescribing education: An updated medical school curriculum from the British Pharmacological Society

British Journal of Clinical Pharmacology, EarlyView.
Aims Prescribing is a complex, essential skill that doctors must acquire to practice medicine safely and effectively. The British Pharmacological Society has historically provided a core curriculum to guide clinical pharmacology and prescribing education in UK medical schools.
Dagan O. Lonsdale, Clare Guilding, Jennifer Koenig, Michael Okorie, Reecha Sofat, Simon Maxwell   +5 more
wiley   +1 more source

Agonist efficiency links binding and gating in a nicotinic receptor

eLife, 2023
Receptors signal by switching between resting (C) and active (O) shapes (‘gating’) under the influence of agonists. The receptor’s maximum response depends on the difference in agonist binding energy, O minus C.
Dinesh C Indurthi, Anthony Auerbach
doaj   +1 more source

Actions of Agonists, Fipronil and Ivermectin on the Predominant In Vivo Splice and Edit Variant (RDLbd, I/V) of the Drosophila GABA Receptor Expressed in Xenopus laevis Oocytes [PDF]

, 2014
Ionotropic GABA receptors are the targets for several classes of insecticides. One of the most widely-studied insect GABA receptors is RDL (resistance to dieldrin), originally isolated from Drosophila melanogaster.
Biggin, P, Buckingham, SD, Lees, K, Musgaard, M, Sattelle, D, Suwanmanee, S   +5 more
core   +3 more sources

Pharmacokinetics and pharmacodynamics of intravenous and oral (S)‐ketamine: Investigating metabolite contribution to subjective effects

British Journal of Clinical Pharmacology, EarlyView.
Aims Oral administration of (S)‐ketamine for treatment‐resistant depression (TRD), as alternative to the registered intranasal or off‐label intravenous administrations, has high potential. However, it is characterized by an extensive first‐pass metabolism, resulting in low (S)‐ketamine exposure and high levels of active metabolites, including (S ...
Marije E. Otto, Gabriël E. Jacobs, Joost C. van Mechelen, Laura G. J. M. Borghans, Johan G. C. van Hasselt, Linda B. S. Aulin   +5 more
wiley   +1 more source

Atypical nicotinic agonist bound conformations conferring subtype selectivity [PDF]

Proceedings of the National Academy of Sciences, 2008
The nicotinic acetylcholine (ACh) receptor (nAChR) plays a crucial role in excitatory neurotransmission and is an important target for drugs and insecticides. Diverse nAChR subtypes with various subunit combinations confer differential selectivity for nicotinic drugs.
Motohiro, Tomizawa, David, Maltby, Todd T, Talley, Kathleen A, Durkin, Katalin F, Medzihradszky, Alma L, Burlingame, Palmer, Taylor, John E, Casida   +7 more
openaire   +2 more sources

Cholinergic regulation of mood: from basic and clinical studies to emerging therapeutics. [PDF]

, 2019
Mood disorders are highly prevalent and are the leading cause of disability worldwide. The neurobiological mechanisms underlying depression remain poorly understood, although theories regarding dysfunction within various neurotransmitter systems have ...
Dulawa, Stephanie C, Janowsky, David S
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