Send to

Choose Destination
Eur J Pharmacol. 2003 Jan 17;459(2-3):217-9.

Naloxone displacement at opioid receptor sites measured in vivo in the human brain.

Author information

Psychopharmacology Unit, School of Medical Sciences, University of Bristol, University Walk, BS8 1TD, Bristol, UK.


We report the use of a sensitive non-tomographic positron detecting system to measure the dose-response curve of naloxone in human brain. [11C]Diprenorphine was administered to normal volunteers in tracer amounts and, 30 min later, various bolus doses of naloxone were given (1.5-160 microg/kg) intravenously and change in [11C]diprenorphine binding monitored over the next 30 min. We found that this method produced results consistent with existing data. It was observed that approximately 13 microg/kg of naloxone ( approximately 1 mg in an 80 kg man) was required to produce an estimated 50% receptor occupation. This is consistent with the clinical dose of naloxone used to reverse opiate overdose (0.4 mg-1.2 mg).

[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center