In this connection, Varenicline, a novel drug that acts as a partial agonist at the nicotinic cholinergic receptor holds particular importance in smoking cessation.
MATERIALS AND METHODS: A primary literature review was conducted, consisting of a PUBMED database search of English language articles using the keywords Varenicline, smoking cessation, and partial agonist alpha4beta2 nicotinic cholinergic receptor.
3]H]nicotine binding to a nicotinic cholinergic receptor
on PC12 cells.
During pregnancy, nicotine stimulates nicotinic cholinergic receptors
in the placenta and fetus, resulting in various deleterious effects.
Nicotinic cholinergic receptors
have been demonstrated on keratinocytes, which may control keratinocyte adhesion and upward migration in the epidermis," Dr.
In a recent pair of studies, we found that perinatal ETS exposure in rhesus monkeys elicits alterations in cell signaling in the developing brain akin to those identified for nicotine administration in rodents, including the up-regulation of nicotinic cholinergic receptors, a characteristic of chronic nicotineinduced neuronal stimulation (Slotkin et al.
Perinatal exposure to environmental tobacco smoke upregulates nicotinic cholinergic receptors in monkey brain.
In addition to inhibiting cholinesterase, CPF, like nicotine, interacts directly with nicotinic cholinergic receptors
(Katz et al.
Physostigmine also can interact directly with nicotinic cholinergic receptors
(50), but one would then expect PC12 cells, which are enriched in these receptors, to be targeted far more than C6 cells, which are not, rather than the converse, as found here.
Studies with cholinergic receptor blocking agents and protein kinase C inhibitors indicated two distinct types of effects, one mediated through stimulation of nicotinic cholinergic receptors and the other targeting intracellular signaling.
Indeed, both chlorpyrifos and chlorpyrifos oxon are capable of direct actions on muscarinic and nicotinic cholinergic receptors, influencing second messenger production (26-28) and ion fluxes (29,30); hence, even some of the cholinotypic actions on developing systems may be mechanistically unrelated to inhibition of cholinesterase activity.