Sequestration also follows short-term exposure but requires drug occupancy and reverses immediately after dissociation of the drug from receptor. However, if the agonist remains coupled for a sufficient period of time (hours), downregulation occurs in which receptor numbers diminish. Interestingly, the ...
The unique physiological, functional and pharmacological characteristics of the α7 nAChR subtype make these receptors prime candidates as drug targets. The canonical signaling mechanism of nAChRs involves the binding of a standard nAChR agonist, such as acetylcholine or nicotine, which induces a ...
The novel α7 nicotinic acetylcholine receptor agonist Neuropsychopharmacology 3060 Encenicline for cognitive impairment in schizophrenia RSE Keefe et al EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens. Psychopharmacology (Berl) 231: 4541–4551. Kay SR...
α7 is a homo-pentamer containing topographically distinct sites for agonists, calcium, and drug modulators with each type of site present in five copies. However, functional relationships between agonist, calcium, and drugmodulator sites remain poorly understood. To investigate these relationships, we...
et al. Metabolism and disposition of varenicline, a selective α4β2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos. 2006;34:121-13016221753Google ScholarCrossref 12. Rose JE, Behm FM, Westman EC, Levin ED, Stein RM, Ripka GV. Mecamylamine combined with...
α-conotoxin MrIC is a biased agonist at α 7 nicotinic acetylcholine receptors. Biochem. Pharmacol. 2015, 94, 155–163. [CrossRef] [PubMed] 79. Dutertre, S.; Nicke, A.; Lewis, R.J. β2 subunit contribution to 4/7 α-conotoxin binding to the nicotinic acetylcholine re...
Discovery of (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-car boxamide (TC-5619), a selective alpha7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders. J Med Chem. 2012;55:9793–809. Article CAS PubMed Google Scholar...
enhances the stability of dlPFC representations, rendering them resistant to distractors [135], consistent with D1R and α2A-AR increasing dlPFC delay-related firing in monkeys described above. Indeed, the widespread use of the α2A-AR agonist, guanfacine, to treat PFC disorders such as ADHD, ...
Upon administration of the α7nAChR agonist, PNU-282987, we measured arterial blood pressure and heart rate and collected frequent blood samples to evaluate serum pH, PO2, PCO2, Na+, K+, and Cl- between 10 minutes before and 60 minutes after drug administration. We did not detect any ...
Nicotinic acetylcholine receptors (nAChRs) in the central nervous system are involved in higher brain function, i.e., memory, cognition, learning, among others. These receptors also exert various pharmacological effects, such as neuroprotection and antin