Your browser version may not work well with NCBI's Web applications. More information here...
1: Eur J Pharmacol. 2000 May 12;396(1):49-52.Click here to read Links

5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor antagonist.

Jones RM, Portoghese PS.

Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 308 Harvard Street S.E., Minneapolis, MN 55455, USA.

5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K(e)=0.04 nM) and an order of magnitude greater selectivity (selectivity ratios >500) than the prototypical kappa-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells afforded pA(2) values that were comparable to the smooth muscle data. In view of the high selectivity and potency of GNTI, it is a potentially valuable pharmacological tool for opioid research.

PMID: 10822054 [PubMed - indexed for MEDLINE]

Patient Drug Information

  • Naltrexone (ReVia® )

    Naltrexone is used along with counseling and social support to help people who have stopped drinking alcohol and using street drugs continue to avoid drinking or using drugs. Naltrexone should not be used to treat people...

  • Source: AHFS Consumer Medication Information