Rivanicline is a neuronalnicotinicreceptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM). It show > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM and IC50 : 26 nM).
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction. Pozanicline selectively activate neuronalnicotinic acetylcholine receptor (nAChR) subtypes, is a no
(S)-PNU-282987 is the absolute stereochemistry form of PNU-282987. PNU 282987, a potent agonist of α7-containing neuronalnicotinic acetylcholine receptors (nAChRs) with Ki of 26 nM for the rat receptor, has negligible activity against α1β1γδ and α3β4 nAC
High affinity and subtype selective α6β2 and α4β2 partial agonist (Ki values are 12 and 26nM for rat α6β2 and α4β2 receptors respectively). Has low affinity for α3β4 and α7 receptors (Ki values are 4.8 and 13 μM for human α3β4 and rat α7 receptors respectively). Stimulates dopamine release from striatal slices in vitro. Attenuates nicotine-induced self-administration and conditional place preference in rats. Sala et al (2013) CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking c Br.J.Pharmacol. 168 835 PMID:22957729 |Riganti et al (2005) Long-term exposure to the new nicotinic antagonist 1,2-bisN-cytisinylethane upregulates nicotinicreceptor subtypes of SH-SY5Y human neuroblastoma cells. Br.J.Pharmacol. 146 1096 PMID:16273122 |Carbonnelle et al (2003) Nitrogen substitution modifies the activity of cytisine on neuronalnicotinicreceptor subtypes. Eur.J.Pharmacol. 471 85 PMID:12818695
ABT-107, a selective α7 neuronalnicotinicreceptor agonist, demonstrates neuroprotective effects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions.