[125i]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors

Martha I. Dávila-García, John L. Musachio, David C. Perry, Yingxian Xiao, Andrew Horti, Edythe D. London, Robert F. Dannals, Kenneth J. Kellar

Research output: Contribution to journalArticle

Abstract

An analog of epibatidine (EB) was synthesized with an iodine atom in the 2 position of the pyridyl ring. This analog, (±)-exo-2-(2-iodo-5-pyridyl)- 7-azabicyclo[2.2.1]heptane (IPH), as well as its two stereoisomers, displayed high affinity for neuronal nicotinic receptors; therefore, radioiodinated IPH, [125I]IPH, was synthesized with specific radioactivities consistently > 1000 Ci/mmol, and its properties as a radioligand for neuronal nicotinic receptors were evaluated. The characteristics of [125I]IPH binding in tissue homogenates appeared to be virtually identical to those reported for [3H]epibatidine binding; but the high specific radioactivity of [125I]IPH greatly facilitated measurements of nicotinic receptors in tissues with relatively low receptor densities and/or where tissues are in limited supply. Autoradiography with [125I]IPH provided clear localization of nicotinic receptors in brain and adrenal gland after film exposure times of ≤2 days. We conclude that [125I]IPH will be a very useful radioligand for the study of neuronal nicotinic receptors in brain and in peripheral ganglia.

Original languageEnglish (US)
Pages (from-to)445-451
Number of pages7
JournalJournal of Pharmacology and Experimental Therapeutics
Volume282
Issue number1
StatePublished - Jul 1 1997

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ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

Cite this

Dávila-García, M. I., Musachio, J. L., Perry, D. C., Xiao, Y., Horti, A., London, E. D., Dannals, R. F., & Kellar, K. J. (1997). [125i]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors. Journal of Pharmacology and Experimental Therapeutics, 282(1), 445-451.