3]H]nicotine binding to a nicotinic cholinergic receptor
on PC12 cells.
Nicotinic cholinergic receptors
have been demonstrated on keratinocytes, which may control keratinocyte adhesion and upward migration in the epidermis," Dr.
SIBIA has an extensive portfolio of proprietary drug discovery targets encompassing gene families encoding voltage and ligand-gated ion channels including voltage-gated calcium channels (VGCCs), nicotinic cholinergic receptors
(nAChRs) and excitatory amino acid receptors (EAARs).
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.