Results 251 to 260 of about 386,471 (278)

Potential Role of Muscarinic Agonists in Alzheimerʼs Disease

Drugs & Aging, 1997
Alzheimer's disease (AD) is a common neurodegenerative disorder and a leading cause of death among the elderly. Recent advances in our understanding of the neurobiology of AD have provided scientific groundwork for the development of potentially more effective and less toxic treatment strategies for the disease.
Laura D. Baker, Eleanor E. Avery, Sanjay Asthana   +2 more
openaire   +3 more sources

Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.

Journal of Medicinal Chemistry, 1998
Muscarinic agonists were tested in two models indicative of clinical antipsychotic activity: conditioned avoidance responding (CAR) in rats and inhibition of apomorphine-induced climbing in mice.
P. Sauerberg, L. Jeppesen, P. Olesen, T. Rasmussen, Michael D B Swedberg, M. Sheardown, A. Fink-Jensen, C. Thomsen, H. Thøgersen, K. Rimvall, J. Ward, D. Calligaro, N. Delapp, F. Bymaster, H. Shannon   +14 more
semanticscholar   +1 more source

Synthesis of azabicyclic pyrazine derivatives as muscarinic agonists and the preparation of a chloropyrazine analogue with functional selectivity at sub-types of the muscarinic receptor

, 1991
The synthesis of quinuclidine and azanorbornyl pyrazine derivatives has yielded highly potent and efficacious muscarinic agonists; chloro-substitution in the pyrazine ring of the quinuclidine analogue resulted in the formation of a derivative with both ...
R. Baker, L. Street, A. Reeve, J. Saunders   +3 more
semanticscholar   +1 more source

Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.

Journal of Medicinal Chemistry, 2001
Selective muscarinic agonists could be useful in the treatment of neurological disorders such as Alzheimer's disease, schizophrenia, and chronic pain. Many muscarinic agonists have been developed, yet most exhibit at best limited functional selectivity ...
W. G. Rajeswaran, Yang Cao, Xi-Ping Huang, M. E. Wroblewski, Tracy Colclough, Selina Lee, Fenghua Liu, Peter I. Nagy, James Ellis, Beth A. Levine, Karl H. Nocka, W. Messer   +11 more
semanticscholar   +1 more source

Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.

Journal of Medicinal Chemistry, 2003
Muscarinic agonists might be useful in the treatment of neurological disorders, including Alzheimer's disease, schizophrenia, chronic pain, and drug abuse.
Yang Cao, Minjia Zhang, Cindy Wu, Selina Lee, M. E. Wroblewski, Trisha Whipple, P. Nagy, K. Takács-Novák, Attila Balázs, S. Tőrös, W. Messer   +10 more
semanticscholar   +1 more source

Characterization of muscarinic agonists in recombinant cell lines

Life Sciences, 1993
Using recombinant CHO cells that express Hm1-Hm5 receptors, reference muscarinic agonists have been characterized with respect to their activity in receptor binding and second messenger assays. In whole cell [3H]-N-methyl scopolamine binding, no agonist was found to be truly subtype selective, although some showed marked differences between several of ...
Anthony Jerome Thomas, Roy D. Schwarz, Juan C. Jaen, Robert E. Davis, Carolyn J. Spencer, Haile Tecle   +5 more
openaire   +3 more sources

Effects of muscarinic agonists in the guinea‐pig prostate

Autonomic and Autacoid Pharmacology, 2007
Summary1 The contractile response to transmural stimulation of the guinea‐pig prostate is largely due to activation of noradrenergic neurons but there is a small contribution from cholinergic neurons. Carbachol and acetylcholine have been reported to act via muscarinic M1cholinoceptors to facilitate contractions produced by neuronal stimulation of the ...
openaire   +3 more sources

Muscarinic agonists and antagonists in schizophrenia: recent therapeutic advances and future directions.

Handbook of Experimental Pharmacology, 2012
A. Bolbecker, A. Shekhar
semanticscholar   +1 more source

Muscarinic agonists acting through M2 acetylcholine receptors stimulate the migration of an NO-sensitive guanylyl cyclase to the plasma membrane of bovine tracheal smooth muscle

Journal of Receptor and Signal Transduction Research, 2010
Fabiola Pláceres Uray, R. D. de Alfonzo, I. D. de Becemberg, M. Alfonzo   +3 more
semanticscholar   +1 more source

Structural Determinants of Muscarinic Agonist Activity

1989
Traditionally, structure-activity relationships (SAR) among muscarinic cholinergic agonists have been derived from dose-effect studies on isolated tissues or in whole animals (Barlow, 1964). In general, in vitro assays are preferable to in vivo assays for studying relations between chemical structure and actual effect (pharmacodynamics).
openaire   +2 more sources