Abstract
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 κ-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 pA2 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. Copyright (C) 2000 Elsevier Science B.V.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 49-52 |
| Number of pages | 4 |
| Journal | European Journal of Pharmacology |
| Volume | 396 |
| Issue number | 1 |
| DOIs | |
| State | Published - May 12 2000 |
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Keywords
- Binding
- Norbinaltorphimine
- κ-Opioid receptor
Cite this
5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist. / Jones, Robert M.; Portoghese, Philip S.
In: European Journal of Pharmacology, Vol. 396, No. 1, 12.05.2000, p. 49-52.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - 5'-Guanidinonaltrindole, a highly selective and potent κ-opioid receptor antagonist
AU - Jones, Robert M.
AU - Portoghese, Philip S.
PY - 2000/5/12
Y1 - 2000/5/12
N2 - 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 κ-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 pA2 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. Copyright (C) 2000 Elsevier Science B.V.
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 κ-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 pA2 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. Copyright (C) 2000 Elsevier Science B.V.
KW - Binding
KW - Norbinaltorphimine
KW - κ-Opioid receptor
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UR - http://www.scopus.com/inward/citedby.url?scp=0034640189&partnerID=8YFLogxK
U2 - 10.1016/S0014-2999(00)00208-9
DO - 10.1016/S0014-2999(00)00208-9
M3 - Article
VL - 396
SP - 49
EP - 52
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1
ER -