![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
Vol. 285, Issue 1, 377-386, April 1998
Institute for Behavioral Genetics, University of Colorado, Boulder,
Colorado
The binding of [3H]epibatidine, an alkaloid isolated from
the skin of an Ecuadorean tree frog, was measured both in brain regions dissected from mouse brain and in tissue sections. Binding to each of
12 brain areas was saturable, but apparently monophasic; no indication
of multiple binding sites was obtained. However, inhibition of
epibatidine binding by nicotine, acetylcholine, methylcarbachol and
cytisine in olfactory bulbs revealed a biphasic pattern consistent with
the presence of two sites differentially sensitive to inhibition by
these nicotinic agonists. Cytisine displayed the greatest difference in
inhibitory potency between the two apparent sites. Subsequent analysis
of the inhibition of epibatidine binding by cytisine in membranes
prepared from 12 brain areas also suggested the presence of two sites
in each brain region. The estimated potency of cytisine at each site
was similar in each brain region. However, the proportion of
[3H]epibatidine binding sites that were more sensitive to
inhibtion by cytisine and those sites less sensitive to inhibition by
this agonist varied markedly among the brain regions. Quantitative autoradiographic analyses of mouse brain revealed pattern of
[3H]epibatidine binding sites less sensitive to
inhibition by cytisine that differed markedly from the pattern obtained
with [3H]nicotine. Among brain regions demonstrating
substantial sites less sensitive to cytisine inhibition were the
accessory olfactory nucleus, medial habenula, interpeduncular nucleus,
fasciculus retroflexus, superior colliculus, inferior colliculus and
the pineal gland. The results indicate that epibatidine binds to at least two distinct nicotinic sites in mouse brain that may represent different nicotinic receptor subtypes, one of which appears to be
identical to that measured by the binding of other agonists such as
nicotine or cytisine.
This article has been cited by other articles:
|
|
 |
|
  L. J. Bierut, J. A. Stitzel, J. C. Wang, A. L. Hinrichs, R. A. Grucza, X. Xuei, N. L. Saccone, S. F. Saccone, S. Bertelsen, L. Fox, et al. Variants in Nicotinic Receptors and Risk for Nicotine Dependence Am J Psychiatry, September 1, 2008; 165(9): 1163 - 1171. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. De Biasi and R. Salas Influence of Neuronal Nicotinic Receptors over Nicotine Addiction and Withdrawal Experimental Biology and Medicine, August 1, 2008; 233(8): 917 - 929. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 P. Whiteaker, M. J. Marks, S. Christensen, C. Dowell, A. C. Collins, and J. M. McIntosh Synthesis and Characterization of 125I-{alpha}-Conotoxin ArIB[V11L;V16A], a Selective {alpha}7 Nicotinic Acetylcholine Receptor Antagonist J. Pharmacol. Exp. Ther., June 1, 2008; 325(3): 910 - 919. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 C. Gotti, M. Moretti, N. M. Meinerz, F. Clementi, A. Gaimarri, A. C. Collins, and M. J. Marks Partial Deletion of the Nicotinic Cholinergic Receptor {alpha}4 or {beta}2 Subunit Genes Changes the Acetylcholine Sensitivity of Receptor-Mediated 86Rb+ Efflux in Cortex and Thalamus and Alters Relative Expression of {alpha}4 and {beta}2 Subunits Mol. Pharmacol., June 1, 2008; 73(6): 1796 - 1807. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. Walsh, A. P. Govind, R. Mastro, J. C. Hoda, D. Bertrand, Y. Vallejo, and W. N. Green Up-regulation of Nicotinic Receptors by Nicotine Varies with Receptor Subtype J. Biol. Chem., March 7, 2008; 283(10): 6022 - 6032. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. I. Damaj, C. Fonck, M. J. Marks, P. Deshpande, C. Labarca, H. A. Lester, A. C. Collins, and B. R. Martin Genetic Approaches Identify Differential Roles for {alpha}4beta2* Nicotinic Receptors in Acute Models of Antinociception in Mice J. Pharmacol. Exp. Ther., June 1, 2007; 321(3): 1161 - 1169. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 X. Guo and R. A. J. Lester Ca2+ Flux and Signaling Implications by Nicotinic Acetylcholine Receptors in Rat Medial Habenula J Neurophysiol, January 1, 2007; 97(1): 83 - 92. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
X. Guo and R. A. J. Lester Regulation of Nicotinic Acetylcholine Receptor Desensitization by Ca2+ J Neurophysiol, January 1, 2007; 97(1): 93 - 101. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. J. Marks, P. Whiteaker, and A. C. Collins Deletion of the {alpha}7, beta2, or beta4 Nicotinic Receptor Subunit Genes Identifies Highly Expressed Subtypes with Relatively Low Affinity for [3H]Epibatidine Mol. Pharmacol., September 1, 2006; 70(3): 947 - 959. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 C. Fonck, B. N. Cohen, R. Nashmi, P. Whiteaker, D. A. Wagenaar, N. Rodrigues-Pinguet, P. Deshpande, S. McKinney, S. Kwoh, J. Munoz, et al. Novel Seizure Phenotype and Sleep Disruptions in Knock-In Mice with Hypersensitive {alpha}4* Nicotinic Receptors J. Neurosci., December 7, 2005; 25(49): 11396 - 11411. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. R. Turner and K. J. Kellar Nicotinic Cholinergic Receptors in the Rat Cerebellum: Multiple Heteromeric Subtypes J. Neurosci., October 5, 2005; 25(40): 9258 - 9265. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T. Darsow, T. K. Booker, J. C. Pina-Crespo, and S. F. Heinemann Exocytic Trafficking Is Required for Nicotine-induced Up-regulation of {alpha}4{beta}2 Nicotinic Acetylcholine Receptors J. Biol. Chem., May 6, 2005; 280(18): 18311 - 18320. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. C. Hernandez, S. Vicini, Y. Xiao, M. I. Davila-Garcia, R. P. Yasuda, B. B. Wolfe, and K. J. Kellar The Nicotinic Receptor in the Rat Pineal Gland Is an {alpha}3{beta}4 Subtype Mol. Pharmacol., October 1, 2004; 66(4): 978 - 987. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
Y. Xiao and K. J. Kellar The Comparative Pharmacology and Up-Regulation of Rat Neuronal Nicotinic Receptor Subtype Binding Sites Stably Expressed in Transfected Mammalian Cells J. Pharmacol. Exp. Ther., July 1, 2004; 310(1): 98 - 107. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. L. Parker, Y. Fu, K. McAllen, J. Luo, J. M. McIntosh, J. M. Lindstrom, and B. M. Sharp Up-Regulation of Brain Nicotinic Acetylcholine Receptors in the Rat during Long-Term Self-Administration of Nicotine: Disproportionate Increase of the {alpha}6 Subunit Mol. Pharmacol., March 1, 2004; 65(3): 611 - 622. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. Cui, T. K. Booker, R. S. Allen, S. R. Grady, P. Whiteaker, M. J. Marks, O. Salminen, T. Tritto, C. M. Butt, W. R. Allen, et al. The {beta}3 Nicotinic Receptor Subunit: A Component of {alpha}-Conotoxin MII-Binding Nicotinic Acetylcholine Receptors that Modulate Dopamine Release and Related Behaviors J. Neurosci., December 3, 2003; 23(35): 11045 - 11053. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. Salas, A. Orr-Urtreger, R. S. Broide, A. Beaudet, R. Paylor, and M. De Biasi The Nicotinic Acetylcholine Receptor Subunit alpha 5 Mediates Short-Term Effects of Nicotine in Vivo Mol. Pharmacol., May 1, 2003; 63(5): 1059 - 1066. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
C. Fonck, R. Nashmi, P. Deshpande, M. I. Damaj, M. J. Marks, A. Riedel, J. Schwarz, A. C. Collins, C. Labarca, and H. A. Lester Increased Sensitivity to Agonist-Induced Seizures, Straub Tail, and Hippocampal Theta Rhythm in Knock-In Mice Carrying Hypersensitive alpha 4 Nicotinic Receptors J. Neurosci., April 1, 2003; 23(7): 2582 - 2590. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
P. Whiteaker, C. G. Peterson, W. Xu, J. M. McIntosh, R. Paylor, A. L. Beaudet, A. C. Collins, and M. J. Marks Involvement of the alpha 3 Subunit in Central Nicotinic Binding Populations J. Neurosci., April 1, 2002; 22(7): 2522 - 2529. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
N. Champtiaux, Z.-Y. Han, A. Bessis, F. M. Rossi, M. Zoli, L. Marubio, J. M. McIntosh, and J.-P. Changeux Distribution and Pharmacology of alpha 6-Containing Nicotinic Acetylcholine Receptors Analyzed with Mutant Mice J. Neurosci., February 15, 2002; 22(4): 1208 - 1217. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. M. Kulak, J. M. McIntosh, and M. Quik Loss of Nicotinic Receptors in Monkey Striatum after 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine Treatment Is Due to a Decline in alpha -Conotoxin MII Sites Mol. Pharmacol., January 1, 2002; 61(1): 230 - 238. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
P. Whiteaker, J. M. McIntosh, S. Luo, A. C. Collins, and M. J. Marks 125I-alpha -Conotoxin MII Identifies a Novel Nicotinic Acetylcholine Receptor Population in Mouse Brain Mol. Pharmacol., May 1, 2000; 57(5): 913 - 925. [Abstract] [Full Text]
|
|
|
|
|
|
A. G. Mukhin, D. Gündisch, A. G. Horti, A. O. Koren, G. Tamagnan, A. S. Kimes, J. Chambers, D. B. Vaupel, S. L. King, M. R. Picciotto, et al. 5-Iodo-A-85380, an alpha 4beta 2 Subtype-Selective Ligand for Nicotinic Acetylcholine Receptors Mol. Pharmacol., March 1, 2000; 57(3): 642 - 649. [Abstract] [Full Text]
|
|
|
|
|
|
D. C. Perry, M. I. Dávila-García, C. A. Stockmeier, and K. J. Kellar Increased Nicotinic Receptors in Brains from Smokers: Membrane Binding and Autoradiography Studies J. Pharmacol. Exp. Ther., June 1, 1999; 289(3): 1545 - 1552. [Abstract] [Full Text]
|
|
|
|
|
|
M. J. Marks, P. Whiteaker, J. Calcaterra, J. A. Stitzel, A. E. Bullock, S. R. Grady, M. R. Picciotto, J.-P. Changeux, and A. C. Collins Two Pharmacologically Distinct Components of Nicotinic Receptor-Mediated Rubidium Efflux in Mouse Brain Require the beta 2 Subunit J. Pharmacol. Exp. Ther., May 1, 1999; 289(2): 1090 - 1103. [Abstract] [Full Text]
|
|
|
|
|
|
M. J. Parker, A. Beck, and C. W. Luetje Neuronal Nicotinic Receptor beta 2 and beta 4 Subunits Confer Large Differences in Agonist Binding Affinity Mol. Pharmacol., December 1, 1998; 54(6): 1132 - 1139. [Abstract] [Full Text]
|
|
|
|
|
|
S. W. Rogers, L. C. Gahring, A. C. Collins, and M. Marks Age-Related Changes in Neuronal Nicotinic Acetylcholine Receptor Subunit alpha 4 Expression Are Modified by Long-Term Nicotine Administration J. Neurosci., July 1, 1998; 18(13): 4825 - 4832. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
