Results 1 to 10 of about 892 (100)

Binding of N-methylscopolamine to the extracellular domain of muscarinic acetylcholine receptors. [PDF]

Sci Rep, 2017
AbstractInteraction of orthosteric ligands with extracellular domain was described at several aminergic G protein-coupled receptors, including muscarinic acetylcholine receptors. The orthosteric antagonists quinuclidinyl benzilate (QNB) and N-methylscopolamine (NMS) bind to the binding pocket of the muscarinic acetylcholine receptor formed by ...
Jakubík J, Randáková A, Zimčík P, El-Fakahany EE, Doležal V.   +4 more
europepmc   +4 more sources

Subtype-selective inhibition of [methyl-3H]-N-methylscopolamine binding to muscarinic receptors by alpha-truxillic acid esters. [PDF]

Br J Pharmacol, 1999
Seven esters of α‐truxillic acid have been synthesized: bis‐3‐piperidylpropyl ester and its quaternary bis‐N‐ethyl derivative, bis‐N‐diethylaminopropyl ester and its quaternary bis‐N‐methyl derivative, and bis‐4‐piperidylbutyl ester and its quaternary bis‐N‐methyl and bis‐N‐ethyl derivatives.
Lysíková M, Fuksová K, Elbert T, Jakubík J, Tucek S.   +4 more
europepmc   +4 more sources

Long-term activation upon brief exposure to xanomleline is unique to M1 and M4 subtypes of muscarinic acetylcholine receptors. [PDF]

PLoS ONE, 2014
Xanomeline is an agonist endowed with functional preference for M1/M4 muscarinic acetylcholine receptors. It also exhibits both reversible and wash-resistant binding to and activation of these receptors.
Eva Šantrůčková, Vladimír Doležal, Esam E El-Fakahany, Jan Jakubík   +3 more
doaj   +1 more source

Subtype differences in pre-coupling of muscarinic acetylcholine receptors. [PDF]

PLoS ONE, 2011
Based on the kinetics of interaction between a receptor and G-protein, a myriad of possibilities may result. Two extreme cases are represented by: 1/Collision coupling, where an agonist binds to the free receptor and then the agonist-receptor complex ...
Jan Jakubík, Helena Janíčková, Alena Randáková, Esam E El-Fakahany, Vladimír Doležal   +4 more
doaj   +1 more source

Assessment of Novel Muscarinic Acetylcholine Receptors in Rat Cerebral Cortex by a Tissue Segment Binding Method

Journal of Pharmacological Sciences, 2010
Muscarinic acetylcholine receptors (mAChRs) of rat cerebral cortex were evaluated using a tissue segment radioligand binding assay. [3H]-Quinuclidinyl benzilate (QNB, a hydrophobic ligand) specifically bound to mAChRs in the cortex segments.
Kung-Shing Lee, Atsushi Nishimune, Hatsumi Yoshiki, Abu Syed Md Anisuzzaman, Fumiko Suzuki, Mao-Hsien Wang, Juei-Tang Cheng, Ikunobu Muramatsu   +7 more
doaj   +1 more source

An Herbal Remedy for the Treatment of Functional Dyspepsia Shows Multi-Target Pharmacological Effects

Natural Product Communications
Objective Herbal medicinal products (HMPs) are commonly used to treat symptoms of mild functional gastrointestinal disorders (FGID) such as functional dyspepsia (FD) and irritable bowel syndrome (IBS).
Nils Günnewich, Kurt Appel, Thorsten Rose, Juan A. Collado Rojas, Eduardo Muñoz, Carsten Tober, Christian Zimmermann   +6 more
doaj   +1 more source

Effect of Sequence of Administration on the Pharmacokinetic In,t. eraction between the Anticholinergic n Drug Biperiden and ['H]Quinuclidinyl Benzylate or [5H]N-Methylscopolamine in Rats

Journal of Pharmacy and Pharmacology, 1998
AbstractIn rats the pharmacokinetic interactions between the anticholinergic drug biperiden and [3H]quinuclidinyl benzylate ([3H]QNB) or [3H]N-methylscopolamine ([3H]NMS) is affected by the sequence in which the drugs are administered.Drug concentrations in various tissues were determined after intravenous administration of [3H]QNB or [3H]NMS (325 ng ...
Junko Ishizaki, Koichi Yokogawa, Emi Nakashima, Tatsunori Takayasu, Tohru Ohshima, Fujio Ichimura   +5 more
openaire   +1 more source

Early central cardiovagal dysfunction after high fat diet in a murine model. [PDF]

Sci Rep, 2023
Strain MM, Espinoza L, Fedorchak S, Littlejohn EL, Andrade MA, Toney GM, Boychuk CR.   +6 more
europepmc   +1 more source

Development of a Selective and High Affinity Radioligand, [³H]VU6013720, for the M₄ Muscarinic Receptor. [PDF]

Mol Pharmacol, 2023
Qi A, Kling HE, Billard N, Rodriguez AL, Peng L, Dickerson JW, Engers JL, Bender AM, Moehle MS, Lindsley CW, Rook JM, Niswender CM.   +11 more
europepmc   +1 more source

Effect of oxidative stress on (3H)N-methylscopolamine binding and production of thiobarbituric acid reactive substances in rat cerebral cortex membranes.

General physiology and biophysics, 1993
We investigated the effect of lipid peroxidation, in vitro induced by H2O2 or FeSO4 and ascorbic acid, on binding properties of muscarinic receptors in rat cerebral cortex membranes. Simultaneously the concentrations of thiobarbituric acid reactive substances (TBARS) were measured to assess the extent of lipid peroxidation.
Z, Kvaltínová, I, Juránek, J, Machová, S, Stolc   +3 more
openaire   +1 more source