Sentences with phrase «partial agonists»

Using sazetidine - A as a template, medicinal chemists developed multiple series of novel ligands with modifications to the pyridine core, azetidine ring, and alkynyl side chain with the objective of designing α4β2 - nAChR partial agonists of high specificity.

Mechanism of AMPA Receptor Activation by Partial Agonists.

Liu, J., Yu, L. F., Eaton, J. B., Caldarone, B., Cavino, K., Ruiz, C., Terry, M., Fedolak, A., Wang, D., Ghavami, A., Lowe, D. A., Brunner, D., Lukas, R. J., Kozikowski, A. P. Discovery of Isoxazole Analogs of Sazetidine - A as Selective alpha4 beta2 - Nicotinic Acetylcholine Receptor (nAChR) Partial Agonists for the Treatment of Depression, Journal of medicinal chemistry 2011 54, 7280 - 7288

The high - affinity nAChR partial agonists varenicline and sazetidine - A exhibit reinforcing properties in rats.

Perhaps partial agonists, directed at these receptor subtypes will have the greatest neuroprotective potential for they would have the ability to inhibit excessive receptor activity without totally shutting down the receptor's ability to perform normal neuronal functions.

The two «frontrunners», according to Dr. Buchanan, are ispronicline (nicotinic receptor partial agonist), and ORG 24448 (modulator of AMPA glutamate receptors).

Yuan, H. T., Khankin, E. V., Karumanchi, S. A. & Parikh, S. M. Angiopoietin 2 is a partial agonist / antagonist of Tie2 signaling in the endothelium.

In contrast, the second angiopoietin ligand, Ang2 acts as partial agonist of Tie2, that is, it inhibits Tie2 signalling in the presence of Ang1 and weakly activates Tie2 in the absence of Ang1 (ref.

Ang2 has been shown to act as partial agonist of Tie2, that is, it is an antagonist of Tie2 activation in the presence of Ang1 and a weak agonist in the absence of Ang1 (ref.

Ang2 is a partial agonist of Tie2 that acts as functional antagonist of Ang1 in Tie2 expressing cells8, 10.

The cannabinoid receptor 1 (CB1) is the principal target of the psychoactive constituent of marijuana, the partial agonist Δ9 - tetrahydrocannabinol (Δ9 - THC).

When an opioid binds to a receptor, it may cause increased receptor activity with a maximum effect (agonist), increased receptor activity that plateaus at an effect lower than maximum (partial agonist), or decreased receptor activity (antagonist).6

Not exact matches

The researchers showed that a two - day treatment regimen with partial or selective PPAR - γ agonists (Telmisartan and Rosiglitazone — both FDA - approved drugs) ameliorated the pathological outcomes of infection in mice by inducing expression of glucose transporters.

We report the crystal structure of a human β2 - adrenergic receptor — T4 lysozyme fusion protein bound to the partial inverse agonist carazolol at 2.4 angstrom resolution.

Partial activation of the yeast pheromone response pathway by beta - adrenergic receptor agonists was achieved in cells coexpressing h beta - AR and a mammalian G protein (Gs) alpha subunit - demonstrating that these components can couple to each other and to downstream effectors when expressed in yeast.

Buprenorphine is a partial mu opioid agonist.

Abstract 12977: Neladenoson, a Partial Adenosine A1 - receptor Agonist, Improves Mitochondrial Function in Left Ventricular Cardiomyocytes Isolated From Dogs With Chronic Heart Failure