Results 191 to 200 of about 13,945 (210)

Clozapine interaction with the M2 and M4 subtypes of muscarinic receptors

European Journal of Pharmacology, 1999
Available evidence indicates that the antipsychotic drug clozapine acts as a partial agonist at the muscarinic M4 and as an antagonist at the M2 receptors. We wondered whether there is indeed a fundamental difference between its action on these two receptor subtypes, and whether it interacts with their classical or allosteric binding sites.
P, Michal, M, Lysíková, E E, El-Fakahany, S, Tucek   +3 more
openaire   +2 more sources

Benzylidene ketal derivatives as M2 muscarinic receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2000
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition.
C D, Boyle, S, Chackalamannil, L Y, Chen, S, Dugar, P, Pushpavanam, W, Billard, H, Binch, G, Crosby, M, Cohen-Williams, V L, Coffin, R A, Duffy, V, Ruperto, J E, Lachowicz   +12 more
openaire   +2 more sources

Interaction of Mg2+ with the allosteric site of muscarinic M2 receptors

Naunyn-Schmiedeberg's Archives of Pharmacology, 1998
Mg2+-ions have been suspected to attenuate the inhibitory effect of allosteric modulators on the dissociation of orthosteric ligands from muscarinic M2 receptors. It was aimed to gain more insight into the molecular events underlying the effect of Mg2+.
U, Burgmer, U, Schulz, C, Tränkle, K, Mohr   +3 more
openaire   +2 more sources

Muscarinic M2 receptor synthesis: study of receptor turnover with propylbenzilylcholine mustard

European Journal of Pharmacology: Molecular Pharmacology, 1995
We have investigated the rate and the functional responsiveness of the newly synthesised M2 muscarinic receptors in HEL 299 cells following propylbenzilylcholine mustard treatment at 37 degrees C. Propylbenzilylcholine mustard induced a dose-dependent loss of the hydrophilic ligand [3H]N-methylscopolamine binding sites with 80% inactivation at 0.1 ...
E B, Haddad, J, Rousell, P J, Barnes
openaire   +2 more sources

Distribution of m2 muscarinic receptors in rat brain using antisera selective for m2 receptors.

Molecular Pharmacology, 1991
The DNA fragment encoding the third intracellular loop of rat m2 muscarinic receptor was fused to the gene for staphylococcal Protein A. The resultant fusion protein, expressed in bacteria, was purified via IgG affinity chromatography and used as an antigen to raise a polyclonal antiserum.
M, Li, R P, Yasuda, S J, Wall, A, Wellstein, B B, Wolfe   +4 more
openaire   +2 more sources

Prejunctional muscarine receptors in the rabbit ear artery differ from M1, M2 and M3 muscarine receptors

Naunyn-Schmiedeberg's Archives of Pharmacology, 1992
The ability of several selective muscarine receptor antagonists to inhibit the effect of carbachol on prejunctional muscarine receptors on sympathetic nerve endings in the rabbit isolated ear artery was investigated to characterise the receptor subtype involved.
S A, Darroch, L K, Choo, F, Mitchelson
openaire   +2 more sources

Characterization of M1- and M2-muscarinic receptors in calf retina membranes

Vision Research, 1988
Muscarinic receptors are identified in bovine retina membranes by the specific binding of 1-[benzilic-4,4'-3H]-quinuclidinyl benzilate [3H]-QNB. Binding occurs to one population of non-cooperative binding sites: KD = 0.11 +/- 0.02 nM and Bmax = 0.61 +/- 0.07 pmol/mg protein.
Vanderheyden, P, Ebinger, G, Vauquelin, G   +2 more
openaire   +3 more sources

Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors

European Journal of Pharmacology, 1996
The interaction of heptane-1,7-bis(dimethyl-3'-phthalimidopropylammonium bromide) (C7/3'-phth), with several agonists, was investigated at the muscarinic M2 receptor in guinea-pig left atria. C7/3'-phth shifted concentration-response curves for the agonists, carbachol, oxotremorine-M and (+)-cis-dioxolane, to the right in a parallel fashion ...
A, Lanzafame, A, Christopoulos, F, Mitchelson   +2 more
openaire   +2 more sources

Methoctramine selectively blocks cardiac muscarinic M2 receptors in vivo

Naunyn-Schmiedeberg's Archives of Pharmacology, 1988
The antimuscarinic effects of methoctramine (N, N'-bis[6-[(2-methoxybenzyl)amino]hexyl]-1, 8-octanediamine tetrahydrochloride), a polymethylene tetraamine endowed with high cardioselectivity in vitro, were assessed in two in vivo preparations. Methoctramine (300 micrograms/kg i.v.) strongly inhibited the methacholine- and muscarine-induced bradycardia ...
J, Wess, P, Angeli, C, Melchiorre, U, Moser, E, Mutschler, G, Lambrecht   +5 more
openaire   +2 more sources

Lack of m2 muscarinic acetylcholine receptor mRNA in rat lymphocytes

Journal of Neuroimmunology, 1994
The presence of muscarinic acetylcholine receptors on lymphocytes has been demonstrated by radioligand binding experiments. Although the specific subtype(s) of muscarinic acetylcholine receptors expressed in lymphocytes is still unknown, some reports suggest the presence of the m2 subtype.
Costa, P, Castoldi, A. F, Traver, D. J, Costa, L. G.   +3 more
openaire   +2 more sources