Results 121 to 130 of about 10,564,162 (159)

Vinburnine decelerates [3H]N-methylscopolamine binding to recombinant human muscarinic M1–M4 acetylcholine receptors

European Journal of Pharmacology, 2004
The kinetics of [3H]N-methylscopolamine binding to membranes of Chinese hamster ovary (CHO) cells expressing muscarinic M(1)-M(4) acetylcholine receptors was studied. [3H]N-methylscopolamine dissociation was used for the "single-point" analysis of allosteric modulation by vinburnine (L-eburnamonine). [3H]N-methylscopolamine dissociation was decelerated
Gabor Maksay, Bela Kiss
exaly   +3 more sources

Kinetics of N-methylscopolamine interaction with muscarinic receptor from rat cerebral cortex

Neurochemistry International, 1989
Kinetics of binding of tritiated N-methylscopolamine with muscarinic receptor from rat cerebral cortex and kinetics of dissociation of this receptor-ligand complex were studied at 25 degrees C. The plot of the observed association rate constants vs the ligand concentration was hyperbolic, giving evidence of a two-step binding mechanism involving a fast
Jaak Jarv, M Eller
exaly   +3 more sources

Influence of pH on the binding of scopolamine and N-methylscopolamine to muscarinic receptors in the corpus striatum and heart of rats.

Molecular Pharmacology, 1990
The influence of pH on the binding of scopolamine and [3H]N-methylscopolamine to muscarinic receptors in the heart and corpus striatum was investigated. The specific binding of [3H]N-methylscopolamine in the heart and corpus striatum was relatively insensitive to pH over the range of 6 through 10 but decreased markedly below pH 6.0.
Frederick J Ehlert
exaly   +3 more sources

Changes of Cooperativity between N-Methylscopolamine and Allosteric Modulators Alcuronium and Gallamine Induced by Mutations of External Loops of Muscarinic M3 Receptors

Molecular Pharmacology, 2001
To clarify the involvement of specific domains of muscarinic receptors in the action of allosteric modulators, muscarinic M(3) receptors (on which allosteric interactions are weak) were genetically modified to become more similar to M(2) receptors (on which allosteric interactions are strong) and were expressed in COS-7 cells.
Alena Krejčí, Stanislav Tuček
exaly   +3 more sources

Multiple binding affinities of N-methylscopolamine to brain muscarinic acetylcholine receptors: differentiation from M1 and M2 receptor subtypes.

Journal of Pharmacology and Experimental Therapeutics, 1986
The properties of the specific binding of the muscarinic receptor ligands [3H]quinuclidinyl benzilate and N-[3H]methylscopolamine in rat brain were compared. The specific binding of both ligands was affected equally by heat, phospholipase A2 and trypsin. N-[3H]methylscopolamine labeled only a fraction of the total muscarinic receptors recognized by [3H]
Esam E El-Fakahany, V Ramkumar
exaly   +3 more sources

Quantitative analysis of binding parameters of [3H]N-methylscopolamine in central nervous system of muscarinic acetylcholine receptor knockout mice

Molecular Brain Research, 2005
We have studied binding parameters (Kd, Bmax) of [3H]N-methylscopolamine ([3H]NMS) in various brain regions and spinal cord of wild-type (WT) and muscarinic acetylcholine receptor (mAChR) subtype (M1-M5) knockout (KO) mice. In the M1-M4 KO mice, the number of [3H]NMS binding sites (Bmax) was decreased throughout the central nervous system (CNS) with ...
Tomomi Oki, Makoto M Taketo, Minoru Matsui   +2 more
exaly   +3 more sources

Antagonism by the diacylglycerol kinase inhibitor R59 022 of muscarinic receptor-mediated cyclic GMP formation and binding of [3HN-methylscopolamine

Biochemical Pharmacology, 1990
R59 022 possessed potent antimuscarinic properties in inhibiting muscarinic agonist-mediated [ 3 H] cyclic GMP response and antagonist binding in mouse neuroblastoma N1E-115 ...
Wi S Lai, Esam E El-Fakahany
exaly   +3 more sources

Modes of allosteric interactions with free and [ 3 H] N -methylscopolamine-occupied muscarinic M 2 receptors as deduced from buffer-dependent potency shifts

Naunyn-Schmiedeberg's Archives of Pharmacology, 2000
Muscarinic M2 acetylcholine receptors contain an allosteric site that is probably located at the entrance of the ligand binding pocket above the orthosteric binding site. With the orthosteric area not occupied, allosteric agents might gain access to this site.
Christian Trankle, Klaus Mohr, Trankle Christian   +2 more
exaly   +3 more sources

Effect of mazindol administration on (3H)-N-Methylscopolamine binding to rat cerebral cortex

Life Sciences, 1992
Mazindol has been shown to produce anorexia in several animal species including humans, and its pharmacological effects may be elicited by blockade of neuronal reuptake of dopamine and norepinephrine. Chronic treatment of rats with mazindol (10 mg/kg daily, p.o.) caused an increase in muscarinic receptor density (Bmax = 874.7 femtomoles/mg protein) as ...
G S, Viana, F C, Sousa, M M, Marinho
openaire   +2 more sources

Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors.

Molecular Pharmacology, 1990
The effect of the neuromuscular blocker alcuronium on the binding of N-[3H]-methylscopolamine [( 3H]NMS) and l-[3H]quinuclidinylbenzilate ([3H]QNB) to muscarinic binding sites in rat heart atria, longitudinal smooth muscle of the ileum, cerebral cortex, cerebellum, and submaxillary glands was measured using filtration techniques. In the presence of 10(-
S, Tucek, J, Musílková, J, Nedoma, J, Proska, S, Shelkovnikov, J, Vorlícek   +5 more
openaire   +2 more sources