Preparation of [11C]buprenorphine--a potential radioligand for the study of the opiate receptor system in vivo.
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.
D000818:Animals; D002047:Buprenorphine / Q000302:isolation & purification / Q000378:metabolism*; D002250:Carbon Radioisotopes / Q000302:isolation & purification / Q000378:metabolism*; D011869:Radioligand Assay; D011957:Receptors, Opioid / Q000378:metabolism*; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D011957:Receptors, Opioid; D002047:Buprenorphine