Comparison of [11C]diprenorphine and [11C]carfentanil in vivo binding to opiate receptors in man using a dual detector system

Victor L. Villemagne; J. James Frost; Robert F. Dannals; John R. Lever; Shuji Tanada; T. K. Natarajan; Alan A. Wilson; Hayden T. Ravert; Henry N. Wagner

doi:10.1016/0014-2999(94)90712-9

Comparison of [¹¹C]diprenorphine and [¹¹C]carfentanil in vivo binding to opiate receptors in man using a dual detector system

Victor L. Villemagne, J. James Frost, Robert F. Dannals, John R. Lever, Shuji Tanada, T. K. Natarajan, Alan A. Wilson, Hayden T. Ravert, Henry N. Wagner

School of Medicine

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

A simple dual detector coincidence system was used to measure the binding of [¹¹C]carfentanil and [¹¹C]diprenorphine to opiate receptors in normal volunteers before and after the administration of naloxone. Total radioactivity without naloxone and the ratio of total/non-specific radioactivity was 2 times greater for [¹¹C]diprenorphine than [¹¹C]carfentanil. The dose of naloxone required to maximally block specific [¹¹C]diprenorphine binding was 10 times that for [¹¹C]carfentanil, indicating that [¹¹C]diprenorphine labels opiate receptor subtypes in addition to μ opiate receptors.

Original language	English (US)
Pages (from-to)	195-197
Number of pages	3
Journal	European Journal of Pharmacology
Volume	257
Issue number	1-2
DOIs	https://doi.org/10.1016/0014-2999(94)90712-9
State	Published - May 12 1994

Keywords

Dual detector system
Opiate receptor
Positron emitting tracer

ASJC Scopus subject areas

Pharmacology

Access to Document

10.1016/0014-2999(94)90712-9

Cite this

Villemagne, V. L., James Frost, J., Dannals, R. F., Lever, J. R., Tanada, S., Natarajan, T. K., Wilson, A. A., Ravert, H. T., & Wagner, H. N. (1994). Comparison of [¹¹C]diprenorphine and [¹¹C]carfentanil in vivo binding to opiate receptors in man using a dual detector system. European Journal of Pharmacology, 257(1-2), 195-197. https://doi.org/10.1016/0014-2999(94)90712-9

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title = "Comparison of [11C]diprenorphine and [11C]carfentanil in vivo binding to opiate receptors in man using a dual detector system",

abstract = "A simple dual detector coincidence system was used to measure the binding of [11C]carfentanil and [11C]diprenorphine to opiate receptors in normal volunteers before and after the administration of naloxone. Total radioactivity without naloxone and the ratio of total/non-specific radioactivity was 2 times greater for [11C]diprenorphine than [11C]carfentanil. The dose of naloxone required to maximally block specific [11C]diprenorphine binding was 10 times that for [11C]carfentanil, indicating that [11C]diprenorphine labels opiate receptor subtypes in addition to μ opiate receptors.",

keywords = "Dual detector system, Opiate receptor, Positron emitting tracer",

author = "Villemagne, {Victor L.} and {James Frost}, J. and Dannals, {Robert F.} and Lever, {John R.} and Shuji Tanada and Natarajan, {T. K.} and Wilson, {Alan A.} and Ravert, {Hayden T.} and Wagner, {Henry N.}",

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AU - Villemagne, Victor L.

AU - James Frost, J.

AU - Dannals, Robert F.

AU - Lever, John R.

AU - Tanada, Shuji

AU - Natarajan, T. K.

AU - Wilson, Alan A.

AU - Ravert, Hayden T.

AU - Wagner, Henry N.

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AB - A simple dual detector coincidence system was used to measure the binding of [11C]carfentanil and [11C]diprenorphine to opiate receptors in normal volunteers before and after the administration of naloxone. Total radioactivity without naloxone and the ratio of total/non-specific radioactivity was 2 times greater for [11C]diprenorphine than [11C]carfentanil. The dose of naloxone required to maximally block specific [11C]diprenorphine binding was 10 times that for [11C]carfentanil, indicating that [11C]diprenorphine labels opiate receptor subtypes in addition to μ opiate receptors.

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KW - Opiate receptor

KW - Positron emitting tracer

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