Binding of narcotic analgesics to plasma and tissues in vitro

Derick H Lau, L. Lim, G. L. Henderson

Research output: Contribution to journalArticlepeer-review


Binding of 3H-fentanyl, 14C-methadone and 3H-l-α-acetyl-methadol (3H-LAAM) to rat plasma and tissues was studied in vitro. Tissue homogenates of brain, lung, heart, liver, kidney and skeletal muscle (10% w/v) were dialysed, at 24°C, against 1.0 μm of each radiolabeled compound in Krebs-Ringer phosphate buffer for 5 hr to reach equilibria. 3H-LAAM was bound more extensively (28-62%) to plasma and tissue homogenates than 14C-methadone (16-57%) which, in turn, was bound more than 3H-fentanyl (16-37%). Liver had the highest affinity for all three drugs whereas muscle and plasma appeared to have the lowest. Other tissues generally had a lower affinity for the three drugs. There was no apparent relationship between the percent of drug bound and the total protein concentration in each tissue. However, for each drug there was a good correlation between the percent drug bound and its octanol/water partition coefficient. The differences in the duration of action between fentanyl, methadone and LAAM may be explained by the differences in their plasma and tissue binding.

Original languageEnglish (US)
JournalFederation Proceedings
Issue number3 I
StatePublished - 1979

ASJC Scopus subject areas

  • Medicine(all)


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