Results 211 to 220 of about 496,043 (271)

Relationships between phosphoinositide and calcium responses to muscarinic agonists in astrocytoma cells.

Molecular Pharmacology, 1984
Activation of muscarinic receptors in human astrocytoma (1321N1) cells stimulates phosphoinositide metabolism and calcium mobilization. The muscarinic effect on phosphoinositide turnover is evidenced by increased formation of [3H]inositol 1-phosphate ...
S. Masters, T. Harden, J. Brown
semanticscholar   +1 more source

Discriminative stimulus properties of muscarinic agonists

Psychopharmacology, 1987
In a two-lever, food-reinforced drug-discrimination paradigm separate groups of rats were trained to discriminate either arecoline, pilocarpine or oxotremorine from saline. The discriminative cues of all three agonists were potently blocked by scopolamine, but only by 30-60 fold higher doses of methylscopolamine.
M, Jung, L, Costa, G T, Shearman, P H, Kelly   +3 more
openaire   +2 more sources

Muscarinic receptor agonists and antagonists

Expert Opinion on Therapeutic Patents, 1999
Although four different subtypes of the muscarinic acetylcholine (ACh) receptor with functional correlates are known to exist (function for M5 is still unclear), all muscarinic agonists and antagon...
Darius P Zlotos, Wiebke Bender, Ulrike Holzgrabe   +2 more
openaire   +1 more source

Striatal muscarinic receptors: Regulation by dopaminergic agonists

Life Sciences, 1981
Abstract The effects of apomorphine on the binding properties of striatal muscarinic receptors were investigated using the specific muscarinic antagonist, [ 3 H](−)3-quinuclidinyl benzilate ([ 3 H](−)QNB). When binding measurements were made in 50 mM sodium/HEPES buffer, pH 7.4, containing Mg +2 , the binding of [ 3 H](−)QNB was consistent with the ...
F J, Ehlert, W R, Roeske, H I, Yamamura
openaire   +2 more sources

Muscarinic agonists in Alzheimer's disease

Life Sciences, 1997
As therapeutic agents, M1 agonists in the short-term may palliate symptoms of AD and improve memory function. In the long-term, M1 agonists have the potential to modify the underlying pathophysiology of AD, and thereby prevent or retard the course of dementia.
openaire   +2 more sources

Quinuclidinone O-Alkynyloximes with muscarinic agonist activity

Bioorganic & Medicinal Chemistry, 2002
A series of quinuclidinone O-alkynyloximes (14-19) were synthesized and evaluated in radioligand displacement assays for binding affinities to M1-M3 muscarinic receptors. Radioligand displacement assays were carried out using [3H] oxotremorine-M and [3H] pirenzepine on rat cortical tissue and [3H] N-methylscopolamine on rat heart and submandibulary ...
Somanadhan, B., Loke, W.-K., Sim, M.-K., Go, M.-L.   +3 more
openaire   +2 more sources

Allosteric Modulators and Selective Agonists of Muscarinic Receptors

Journal of Molecular Neuroscience, 2006
Allosteric modulators of ligand-receptor interactions are found for a variety of receptors (Christopoulos, 2002). Allosteric agents attach to a binding site being topographically distinct from the site for conventional (orthosteric) agonists or antagonists.
U. HOLZGRABE, M. DE AMICI, K. MOHR
openaire   +3 more sources

Action of the muscarinic toxin MT7 on agonist-bound muscarinic M1 receptors.

European Journal of Pharmacology, 2004
The muscarinic toxin MT7 is the most selective ligand for the muscarinic M(1) receptors. Previous studies have shown that the toxin interacts with the antagonist-receptor complex and slows the antagonist dissociation rate, possibly by binding to an allosteric site and impeding the access to and egress from the orthosteric binding pocket. In the present
OLIANAS, MARIA CONCETTA, ADEM A, KARLSSON E, ONALI, PIER LUIGI   +3 more
openaire   +2 more sources

Evaluation of Muscarinic Agonist-Induced Analgesia in Muscarinic Acetylcholine Receptor Knockout Mice

Molecular Pharmacology, 2002
Centrally active muscarinic agonists display pronounced analgesic effects. Identification of the specific muscarinic acetylcholine receptor (mAChR) subtype(s) mediating this activity is of considerable therapeutic interest. To examine the roles of the M(2) and M(4) receptor subtypes, the two G(i)/G(o)-coupled mAChRs, in mediating agonist-dependent ...
Alokesh, Duttaroy, Jesus, Gomeza, Jai-Wei, Gan, Nasir, Siddiqui, Anthony S, Basile, W Dean, Harman, Philip L, Smith, Christian C, Felder, Allan I, Levey, Jürgen, Wess   +9 more
openaire   +2 more sources

Molecular mechanics calculations on muscarinic agonists

Journal of Molecular Structure, 1990
Abstract Molecular mechanics calculations have been performed on the conformation freedom with respect to the torsion angles OCCN and COCC of acetylcholine, α( r -methylacetylcholine,β( s )-methylacetylcholine, α( r ),β( s )-diemthylacetylcholine and muscarine, in order to obtain information about the active conformation and its interaction with the ...
Huub Kooijman, Jan A. Kanters, Jan Kroon
openaire   +1 more source