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In vivo labeling of sigma receptors in mouse brain with [3H]4-phenyl-1-(4-phenylbutyl)piperidine

✍ Scribed by Kenji Hashimoto; Ursula Scheffel; Edythe D. London

Publisher
John Wiley and Sons
Year
1995
Tongue
English
Weight
568 KB
Volume
20
Category
Article
ISSN
0887-4476

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✦ Synopsis

4-Pheny1-144-phenylbutyl)piperidine (4-PPBP) is a very potent ligand for u (Sigma) receptors. The present study was undertaken to evaluate l3H14-PPBP as a radioligand for in vivo labeling of cerebral u receptors. After intravenous administration of l3H14-PPBP to mice, there is high uptake of radioactivity in the brain. The regional distribution of radioactivity in the brain 2 h after intravenous injection of I3H14-PPBP parallels the in vitro binding of the radioligand in rat brain (pondmedulla > cerebellum a prefrontal cortex 3 parietal cortex > hypothalamus > olfactory tubercle 3 thalamus > hippocampus > striatum). Pretreatment with haloperidol (2 mg/ kg) significantly decreases the radioactivity measured in the brain 30-120 min after injection of r3H14-PPBP. Pretreatment with unlabeled 4-PPBP or ifenprodil also significantly decreases radioactivity in the brain 2 h after injection of I3H14-PPBP, in a dosedependent manner. The in vivo binding of ['H14-PPBP in the brain also is significantly inhibited by SL 82.0715, BMY 14802, 1,3-di-o-tolylguanidine (DTG), and (+)-enantiomers of pentazocine, SKF 10,047, and 3-PPP, but not by the corresponding (-)-enantiomers, consistent with stereoselectivity of inhibition obtained in in vitro binding studies. In contrast, pretreatment with dizocilpine and spiperone does not inhibit in vivo binding of L3H]4-PPBP. The results indicate that K3H14-PPBP would be a suitable radioligand for in vivo labeling of u receptors in brain. o 1995 Wiley-Liss, Inc.*

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