Results 141 to 150 of about 10,564,162 (159)

Contribution of Lateral Substituents in Symmetrical and Non‐symmetrical Heptane‐bisammonio Compounds to the Allosteric Stabilization of N‐methylscopolamine Binding to Muscarinic M₂ Receptors

Archiv der Pharmazie, 2003
AbstractAllosteric modulators are able to enhance or decrease the equilibrium binding of orthosteric agonists or antagonists. The treatment of Alzheimer's disease and the organophosphorus poisoning can take advantage of the enhancement of the ligand binding.
Markus, Staudt, Christian, Tränkle, Klaus, Mohr, Ulrike, Holzgrabe   +3 more
openaire   +2 more sources

[3H]N-methylscopolamine binding to muscarinic receptors in human peripheral blood lymphocytes: Characterization, localization on T-lymphocyte subsets and age-dependent changes

Neuropharmacology, 1989
The properties of the binding of the muscarinic receptor ligands, [3H]quinuclidinyl benzilate ([3H]QNB) and [3H]N-methylscopolamine ([3H]NMS) in human mononuclear cells were compared. The binding of [3H]QNB showed a high, non-specific component and lack of saturability in both intact mononuclear cells and preparations of lysed mononuclear cell ...
C, Eva, P, Ferrero, P, Rocca, A, Funaro, B, Bergamasco, L, Ravizza, E, Genazzani   +6 more
openaire   +2 more sources

Kinetic studies of [3H]-N-methylscopolamine binding to muscarinic receptors in the rat central nervous system: evidence for the existence of three classes of binding sites.

Molecular Pharmacology, 1986
We compared the binding of [N-methyl-3H]scopolamine methyl chloride [( 3H]NMS) and pirenzepine to muscarinic receptors in four regions of the rat central nervous system (cortex, hippocampus, striatum, and cerebellum) and in rat heart. Equilibrium binding studies suggested the existence of three classes of receptors: A, receptors with high affinity for ...
Waelbroeck, Magali, Gillard, Michel, Robberecht, Patrick, Christophe, Jean   +3 more
openaire   +3 more sources

Allosteric Site on Muscarinic Acetylcholine Receptors: Identification of Two Amino Acids in the Muscarinic M2 Receptor That Account Entirely for the M2/M5 Subtype Selectivities of Some Structurally Diverse Allosteric Ligands in N-Methylscopolamine-Occupied Receptors

Molecular Pharmacology, 2003
Two epitopes have been identified recently to be responsible for the high-affinity binding of alkane-bisammonium and caracurine V type allosteric ligands to N-methylscopolamine (NMS)-occupied M2 muscarinic acetylcholine receptors, relative to M5 receptors: the amino acid M2-Thr423 at the top of transmembrane region (TM) 7 and an epitope comprising the ...
Uta, Voigtländer, Kirstin, Jöhren, Marion, Mohr, Alexandra, Raasch, Christian, Tränkle, Stefan, Buller, John, Ellis, Hans-Dieter, Höltje, Klaus, Mohr   +8 more
openaire   +2 more sources

Affinities of muscarinic drugs for [3H]N-methylscopolamine (NMS) and [3H]oxotremorine (OXO) binding to a mixture of M1−M4 muscarinic receptors: Use of NMS/OXO-M ratios to group compounds into potential agonist, partial agonist, and antagonist classes

Neurochemical Research, 1995
The relative affinities of various muscarinic drugs in the antagonist ([3H]N-methyl scopolamine ([3H]NMS)) and agonist ([3H]Oxotremorine-m ([3H]OXO-M)) binding assays using a mixture of tissues containing M1-M4 receptor subtypes have been determined. [3H]NMS bound with high affinity (Kd = 25 +/- 5.9 pM; n = 3) and to a high density Bmax = 11.8 +/- 0 ...
N A, Sharif, G W, Williams, L M, DeSantis   +2 more
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[³H]N‐Methylscopolamine Binding Studies Reveal M₂ and M₃ Muscarinic Receptor Subtypes on Cerebellar Granule Cells in Primary Culture

Journal of Neurochemistry, 1990
Abstract: Saturation experiments with the muscarinic antagonist [3H]N‐methylscopolamine ([3H]NMS) indicated that cerebellar granule cells in primary culture possess a high density of muscarinic acetylcholine receptors (mAChRs): Bmax= 1.85 ± 0.01 pmol/mg of protein at 10 days in culture; KD= 0.128 ± 0.01 nM The selective M1 antagonist pirenzepine ...
R, Alonso, M, Didier, P, Soubrie
openaire   +2 more sources

Effect of sequence of administration on the pharmacokinetic interaction between the anticholinergic drug biperiden and [3H]quinuclidinyl benzylate or [3H]N-methylscopolamine in rats.

The Journal of pharmacy and pharmacology, 1998
In 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 kg(-1)).
J, Ishizaki, K, Yokogawa, E, Nakashima, T, Takayasu, T, Ohshima, F, Ichimura   +5 more
openaire   +1 more source

3H-N-methylscopolamine binding to human lymphocytes. A model to study cholinergic dysfunction in Alzheimer's disease

Pharmacological Research Communications, 1988
C. Eva, P. Rocca, P. Ferrero, B. Bergamasco, L. Ravizza, E. Genazzani   +5 more
openaire   +1 more source

Potentiation of the action of N-methylscopolamine in guinea pig atria by the allosteric antagonists tetra-W84, W84, and alcuronium

Life Sciences, 1995
A. Maaβ, E. Kostenis, U. Holzgrabe, K. Mohr   +3 more
openaire   +1 more source

Roles of external loops of muscarinic receptors in interactions between N-methylscopolamine and allosteric modulators

2004
Stanislav Tu_ek, Alena Krej_í, Michaela Lysíková, Jan Jakubík, Vladimír Dole_al   +4 more
openaire   +1 more source