Results 221 to 230 of about 32,846 (260)

HM74a Agonists: Will they be the New Generation of Nicotinic Acid?

Current Topics in Medicinal Chemistry, 2009
The discovery of HM74a as a high affinity receptor for nicotinic acid has opened up new areas for investigation. Since its discovery, several new chemical entities have been reported as HM74a agonists. One of them, MK-0354, has been tested in phase II studies, but despite significant decreases in Free Fatty Acid levels with absence of flushing events ...
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Neuronal Nicotinic Acetylcholine Receptor Agonists

Current Pharmaceutical Design, 1996
In contrast to the considerable effort over many years to design agonists of the muscanmc acetylcholine receptor, until recently little attention has been directed towards agonists of the nicotinic family of acetylcholine receptors (NAChRs). Nevertheless, the structure and function of NAChRs has been a topic of intense research for several decades ...
Ian A. McDonald, Jean-Michel Vernier, Nicholas Cosford, Janis Corey-Naeve   +3 more
exaly   +2 more sources

Epibatidine, a potent analgetic and nicotinic agonist.

Molecular Pharmacology, 1994
Synthetic (+)- and (-)-epibatidine (an alkaloid originally characterized from frog skin) have potent analgetic activity in mice, using the hot-plate assay. The natural (+)-enantiomer, with an ED50 of about 1.5 micrograms/kg upon intraperitoneal injection, is about 2-fold more potent than the (-)-enantiomer.
B, Badio, J W, Daly
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Agonist efficiency in a nicotinic receptor

Biophysical Journal, 2023
Dinesh Indurthi, Anthony Auerbach
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Epibatidine, a novel nicotinic receptor agonist

1994
It is speculated that nicotine receptor ligands might be of therapeutic benefit for the treatment of obesity, anxiety, and memory loss. With the exception of nicotine, few selective high-affinity agents exist. (-)Epibatidine (1), isolated from Ecuadoran frogs, shows structural resemblence to (-)nicotine (2). Molecular modeling studies reveal that the N
M. Dukat, D. Dumas, M. I. Damaj, W. Glassco, E. L. May, B. R. Martin, R. A. Glennon, D. M. Wypij, T. Y. Shen, K. R. Creasy, J. Rosecrans, J. P. Sullivan, A. W. Bannon, D. Donnelly-Roberts, D. J. Anderson, M. Piattoni-Kaplan, M. Gopalakrishnan, M. W. Decker, S. P. Arneric, R. Loring, T. McHugh, X. Zhang, J. McKay   +22 more
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Nicotinic Acid Receptor Agonists

Journal of Medicinal Chemistry, 2008
P Douglas, Boatman, Jeremy G, Richman, Graeme, Semple   +2 more
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Agonists and Antagonists of Nicotinic Acetylcholine Receptors

2000
The natural alkaloids nicotine and muscarine (Fig. 1) were the key pharmacologic tools that uncovered the two families of acetylcholine (ACh) receptors in the CNS. These families were defined by the action of these alkaloids to mimic the multiplicity of effects of ACh as a mediator of synaptic transmission (TAYLOR 1996).
S. P. Arneric, M. W. Holladay
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ABT — 418, a Novel Nicotinic Agonist

1994
With the plethora of receptor targets evolving as the result of nicotinic acetylcholine receptor (nAChR) cloning it is possible that new molecular entities selective for subtypes of nAChRs can be developed which are potentially free of the side effect liabilities associated with (-)-nicotine.
S. P. Arneric, M. Williams, M. W. Holladay, J. T. Wasicak, D. Donnelly-Roberts, D. J. Anderson, P. Pavlik, Y. C. Martin, D. S. Garvey, J. P. Sullivan, G. Wilkie, Susan Wonnacott, S. F. Robinson, James R. Pauly, M. W. Decke, J. D. Brioni, M. J. Buckley, P. Curzon, A. B. O’Neill, D. J. B. Kim, M. Majchrzak, K. Marsh, S. Quigley, A. D. Rodrigues, R. Radek, J. J. Buccafusco, W. J. Jackson, A. V. Terry, K. C. Marsh, M. W. Decker, S. P. Amend, J. R. Pauly   +31 more
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Modulation of nicotine receptors by chronic exposure to nicotinic agonists and antagonists.

Ciba Foundation symposium, 1990
Although numerous studies have demonstrated that chronic nicotine treatment often results in tolerance to this drug, the mechanisms that underlie this tolerance are not well defined. Recent evidence suggests that chronic nicotine treatment results in an up-regulation of brain nicotinic receptors, but the majority of these receptors may be desensitized ...
A C, Collins, R V, Bhat, J R, Pauly, M J, Marks   +3 more
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Nicotinic agonist and antagonist effects on memory

Drug Development Research, 1996
Nicotine has been found by a variety of investigators to improve memory in rats, monkeys, and humans. Recent studies have helped to determine the behavioral and pharmacological nature of critical nicotine effects on memory function. Other nicotinic agonists, including ABT-418, GTS-21, or lobeline, can also significantly improve memory performance ...
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