External monitoring of cerebral nicotinic acetylcholine receptors in living mice

The present report describes the feasibility of using a simple procedure for labeling and monitoring nAChRs in the mouse brain. Epibatidine (exo-2-(6-chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane), an alkaloid first isolated from the skin of the Ecuadoran frog Epipedobates tricolor has extremely high...

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Veröffentlicht in:	Synapse (New York, N.Y.) N.Y.), 1997-12, Vol.27 (4), p.378-380
Hauptverfasser:	Liu, Xiang, Musachio, John L., Wagner Jr, Henry N., Mochizuki, Takao, Dannals, Robert F., London, Edythe D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analysis of Variance Animals Brain - diagnostic imaging Feasibility Studies Iodine Radioisotopes Male Mice Mice, Inbred Strains Molecular Structure Radionuclide Imaging Receptors, Nicotinic - analysis
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Zusammenfassung:	The present report describes the feasibility of using a simple procedure for labeling and monitoring nAChRs in the mouse brain. Epibatidine (exo-2-(6-chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane), an alkaloid first isolated from the skin of the Ecuadoran frog Epipedobates tricolor has extremely high affinity for nAChRs. Here we report that the probe system and a radioiodinated analogue of epibatidine, ( plus or minus )-exo-2-(2-[ super(125)I]iodo-5-pyridyl)-7-azabicyclo[2.2.1]heptane ([ super(125)I]IPH) can be used to assess brain nAChRs in living mice. In vitro assays have shown that this tracer has high affinity for nAChRs (K sub(d) = 90 pM in preparations of rat brain membranes), and autoradiography with [ super(125)I]IPH demonstrated clear localization of nAChRs in brain and adrenal gland.
ISSN:	0887-4476 1098-2396
DOI:	10.1002/(SICI)1098-2396(199712)27:4<378::AID-SYN11>3.0.CO;2-O