PMID- 10822054
OWN - NLM
STAT- MEDLINE
DCOM- 20000801
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 396
IP  - 1
DP  - 2000 May 12
TI  - 5'-Guanidinonaltrindole, a highly selective and potent kappa-opioid receptor 
      antagonist.
PG  - 49-52
AB  - 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.
FAU - Jones, R M
AU  - Jones RM
AD  - Department of Medicinal Chemistry, College of Pharmacy, University of Minnesota, 
      308 Harvard Street S.E., Minneapolis, MN 55455, USA.
FAU - Portoghese, P S
AU  - Portoghese PS
LA  - eng
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 
      (17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan)
RN  - 0 (Guanidines)
RN  - 0 (Ligands)
RN  - 0 (Morphinans)
RN  - 0 (Receptors, Opioid, kappa)
RN  - 100929-53-1 (Enkephalin, Ala(2)-MePhe(4)-Gly(5)-)
RN  - 5S6W795CQM (Naltrexone)
RN  - 88373-73-3 (Enkephalin, D-Penicillamine (2,5)-)
SB  - IM
MH  - Animals
MH  - CHO Cells
MH  - Cricetinae
MH  - Enkephalin, Ala(2)-MePhe(4)-Gly(5)-/pharmacology
MH  - Enkephalin, D-Penicillamine (2,5)-/pharmacology
MH  - Guanidines
MH  - Guinea Pigs
MH  - Humans
MH  - In Vitro Techniques
MH  - Ligands
MH  - Male
MH  - Membranes/drug effects/metabolism
MH  - Mice
MH  - Mice, Inbred ICR
MH  - Morphinans
MH  - Muscle, Smooth/drug effects
MH  - Naltrexone/*analogs & derivatives/pharmacology
MH  - Receptors, Opioid, kappa/agonists/*antagonists & inhibitors
EDAT- 2000/05/24 09:00
MHDA- 2000/08/06 11:00
CRDT- 2000/05/24 09:00
PHST- 2000/05/24 09:00 [pubmed]
PHST- 2000/08/06 11:00 [medline]
PHST- 2000/05/24 09:00 [entrez]
AID - S0014-2999(00)00208-9 [pii]
AID - 10.1016/s0014-2999(00)00208-9 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 2000 May 12;396(1):49-52. doi: 10.1016/s0014-2999(00)00208-9.