Preparation of [11C]buprenorphine--a potential radioligand for the study of the opiate receptor system in vivo

Int J Rad Appl Instrum A. 1987;38(1):65-6. doi: 10.1016/0883-2889(87)90239-5.

Abstract

A method is described for the preparation of [11C]buprenorphine in high specific activity, based on the reaction of N-(de-cyclopropylmethyl)buprenorphine with "no carrier added" [1-11C]cyclopropanecarbonyl chloride followed by reduction with lithium aluminium hydride. The [1-11C]cyclopropanecarbonyl chloride is itself prepared from cyclotron-produced [11C]carbon dioxide. The overall preparation time is 57 min from the end of radionuclide production, and the radiochemical yield is ca 20%, (decay-corrected from [11C]-carbon dioxide). [11C]Buprenorphine has potential as a radioligand for the study of the opiate receptor system in vivo by means of position emission tomography.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Buprenorphine / isolation & purification
  • Buprenorphine / metabolism*
  • Carbon Radioisotopes / isolation & purification
  • Carbon Radioisotopes / metabolism*
  • Radioligand Assay
  • Receptors, Opioid / metabolism*
  • Tomography, Emission-Computed

Substances

  • Carbon Radioisotopes
  • Receptors, Opioid
  • Buprenorphine