GR89,696: A Potent κ-Opioid Agonist with Subtype Selectivity in Rhesus Monkeys
GR89,696 is a synthetic κ-opioid receptor agonist, recently reported to have an agonist profile consistent with selectivity at the proposed âκ 2 â subtype. The present studies evaluated the effects of GR89,696 in vitro {i.e., in radioligand binding and [ 35 S]guanosine-5â²- O -(3-thio)triphos...
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Published in | The Journal of pharmacology and experimental therapeutics Vol. 298; no. 3; p. 1049 |
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Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
American Society for Pharmacology and Experimental Therapeutics
01.09.2001
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Online Access | Get full text |
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Summary: | GR89,696 is a synthetic κ-opioid receptor agonist, recently reported to have an agonist profile consistent with selectivity
at the proposed âκ 2 â subtype. The present studies evaluated the effects of GR89,696 in vitro {i.e., in radioligand binding and [ 35 S]guanosine-5â²- O -(3-thio)triphosphate assays} and in vivo in rhesus monkeys, in assays used to study κ-opioid agonists (i.e., thermal antinociception,
sedation and muscle relaxation, diuresis, and increases in serum prolactin levels, as well as ethylketocyclazocine and U69,593
discrimination). Furthermore, the sensitivity of GR89,696 to naltrexone and nor-binaltorphimine (nor-BNI) antagonism was compared
with that of U50,488 and U69,593, ligands selective for the proposed âκ 1 â subtype. Overall, GR89,696 displayed the profile of a highly potent κ-opioid agonist, following parenteral administration
in rhesus monkeys. GR89,696 was less sensitive than U50,488 and U69,593 to naltrexone or nor-BNI antagonism, consistent with
an action through the proposed κ 2 receptor subtype. |
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ISSN: | 0022-3565 1521-0103 |