Rapastinel (GLYX-13) is an investigational intravenous formulation of a novel NMDA receptor partial agonist
, which is being evaluated for adjunctive treatment of MDD, and has shown a rapid onset of antidepressant efficacy 1 day after a single dose in a Phase 2 clinical trial of patients with MDD who had an inadequate response to one or more antidepressants.
The second class comprises the partial agonists
(1 [micro]M [less than or equal to] [K.
Relevance of Vilazodone's 5-HT1A receptor partial agonist
Researchers have studied the effects of dopamine partial agonists
(1)-agents that block the activities of the dopamine receptors (i.
Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist
, vs sustained-release bupropion and placebo for smoking cessation: a randomized controlled trial.
Moreover, efficacy of aripiprazole is mediated through a combination of partial agonist
activity at D2 and 5-HT1A receptors and antagonist activity at 5-HT2A receptors.
At lower concentrations, the difference between GCA and TEF approaches depended on the efficacy of the partial agonist
Because it is a partial agonist
, with increasing dose the effects plateau, making it safer and less likely to result in accidental overdose than full agonists.
D-cycloserine, a NMDA receptor partial agonist
, is currently approved for other uses, but is expected to be used at a substantially lower dosage in the treatment of anxiety disorders.
Varenicline is pharmacologically known as an alpha4beta2 nicotinic acetylcholine receptor partial agonist
, which means that it activates the brain's nicotinic receptors in a manner similar to nicotine, but with less affinity (effect).
There are two possible explanations for this finding: tamoxifen resistance might be overcome by a change in treatment; or aromatase inhibitors might simply be a better treatment option, since they reduce peripheral estrogen concentrations to extremely low levels, whereas tamoxifen is a partial agonist
," wrote the investigators, who were led by Raimund Jakesz, M.
Food and Drug Administration (FDA) for cariprazine, a potent dopamine D3/D2 receptor partial agonist
with preferential binding to D3 receptors.