Kenneth J. Kellar
Professor of Pharmacology
The Ohio State University, 1974
Research in my
laboratory is focused on understanding the structure, function
and regulation of neuronal nicotinic cholinergic receptors in
the brain and the autonomic nervous system. In the brain, these
receptors are strategically located where they can mediate the
release of several important neurotransmitters, including
dopamine, norepinephrine, acetylcholine, GABA and glutamate. In
the autonomic nervous system, nicotinic receptors mediate fast
excitatory transmission at ganglia; therefore, these ganglionic
nicotinic receptors influence the function of nearly all
receptors are composed of two or more protein subunits and exist
as several different receptors subtypes based on their subunit
composition. A major goal of our group's research is to
understand how these receptor subtypes differ with regard to
their specific location within the brain, their pharmacology,
and their regulation. To do this, we employ a wide variety of
techniques, including radioligand binding with ligands selective
for subgroups of these receptors, immunoprecipitation of labeled
receptors and western blot analysis of specific subunits using
selective antibodies, and pharmacological characterization of
receptor functions. We have used molecular biological methods
to create a library of mammalian cells that stably express
neuronal nicotinic receptors of defined subunit composition.
These cells have allowed us to compare the pharmacological
properties of these defined receptor subtypes with native
neuronal receptors in CNS and ganglia.
Hussmann GP, Yasuda RP, Wolfe BB, Xiao, Y, Kellar KJ
Endogenously expressed muscarinic receptors in HEK293 cells augment
up-regulation of stably expressed alpha4-beta2 nicotinic receptors.
J Biol. Chem. 286:39726, 2011
Rezvani AH, Cauley M, Sexton H, Xiao Y, Brown ML, Paige MA, McDowell BE, Kellar KJ, Levin ED.
Sazetidine-A, a selective α4β2 nicotinic
acetylcholine receptor ligand: effects on dizocilpine and
scopolamine-induced attentional impairments in female Sprague-Dawley rats.
Psychopharmacology (Berl). Jan 28 2011. [Epub ahead of print]
- Lomazzo E, MacArthur L, Yasuda RP,
Wolfe BB, Kellar KJ:
Quantitative analysis of the heteromeric neuronal
nicotinic receptors in the rat hippocampus. J Neurochem 115:
- Rezvani AH, Slade S, Wells C, Petro A, Lumeng L, Li TK, Xiao Y,
Brown ML, Paige MA, McDowell BE, Rose JE, Kellar KJ, Levin ED:
Effects of sazetidine-A, a selective alpha4beta2 nicotinic acetylcholine
receptor desensitizing agent on alcohol and nicotine self-administration
in selectively bred alcohol-preferring (P) rats.
- Saba W, Valette H, Granon S, Xiao Y, Kellar KJ, Doll¨¦ F, Bottlaender
[18F]ZW-104, a new radioligand for imaging alpha2-alpha3-alpha4/beta2
central nicotinic acetylcholine receptors: Evaluation in mutant mice.
64:570-2, 2010 No abstract available.
- Levin ED, Rezvani AH, Xiao Y, Slade S, Cauley M, Wells C, Hampton D,
Petro A, Rose JE, Brown ML, Paige MA, McDowell BE, Kellar KJ:
Sazetidine-A, a selective alpha4beta2 nicotinic receptor desensitizing
agent and partial agonist, reduces nicotine self-administration in rats.
J Pharmacol Exp Ther. 332:933-9, 2010
- Valette H, Xiao Y, Peyronneau MA, Damont A, Kozikowski AP, Wei ZL,
Kassiou M, Kellar KJ, Doll¨¦ F, Bottlaender M:
18F-ZW-104: a new radioligand for imaging neuronal nicotinic
acetylcholine receptors--in vitro binding properties and PET studies in
baboons. J Nucl Med.
- Xiao Y, Abdrakhmanova GR, Baydyuk M, Hernandez S, Kellar KJ Rat neuronal nicotinic acetylcholine receptors containing alpha7 subunit:
pharmacological properties of ligand binding and function.
Sin. 30:842-50, 2009
- Cucchiaro G, Xiao Y, Gonzalez-Sulser A, Kellar KJ. Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology
- Cox BC, Marritt AM, Perry DC, Kellar
Transport of multiple nicotinic acetylcholine receptors in the rat optic
nerve: high densities of receptors containing alpha6 and beta3 subunits. J Neurochem.
- Mao D, Perry DC,
Yasuda RP, Wolfe BB, Kellar KJ.
The alpha4beta2alpha5 nicotinic cholinergic receptor in rat brain is
resistant to up-regulation by nicotine in vivo. J Neurochem.
- Perry DC, Mao D, Gold AB, McIntosh JM,
Pezzullo JC, Kellar KJ.
Chronic nicotine differentially regulates alpha6- and beta3-containing
nicotinic cholinergic receptors in rat brain. J Pharmacol. Exp. Ther.
- Ortinski PI, Turner JR, Barberis A,
Motamedi G, Yasuda RP, Wolfe BB, Kellar KJ, Vicini S.Deletion of the GABA(A) receptor alpha1 subunit increases tonic GABA(A)
receptor current: a role for GABA uptake transporters. J Neurosci.
- Kellar KJ.
Proc Natl Acad Sci USA; 103:13263-4, 2006
- Mao D, Yasuda RP, Fan H, Wolfe BB, Kellar
Heterogeneity of nicotinic cholinergic receptors in rat superior
cervical and nodose Ganglia.
Mol Pharmacol. 70:1693-9, 2006
Y, Fan H, Musachio JL, Wei ZL, Chellappan SK, Kozikowski AP, Kellar KJ.
Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic
acetylcholine receptors without activating them. Mol
Pharmacol. 70:1454-60, 2006
- Turner JR, Kellar KJ.
Nicotinic cholinergic receptors in the rat cerebellum: multiple
J Neurosci. 25:9258-65, 2005
- Marritt AM, Cox BC, Yasuda RP, McIntosh JM, Xiao Y,
Wolfe BB, Kellar KJ.
Nicotinic cholinergic receptors in the rat retina: simple and mixed