The potent d-opioid receptor antagonist H-2X,6- . . L-tyrosine Dmt -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid Tic-OH exhibited .w35 partial inverse agonism EC50s6.35 nM, Emaxsy18.87% for SxGTPgS binding and H-Dmt–Tic-NH2 was a neutral antagonist no effect up to 30 mM.. In contrast N,NCH3.2-Dmt–Tic-NH2 was a full inverse agonist EC50s2.66 nM, Emaxsy35.95%. similar to ICI 174864 wN,N-diallyl-Tyr1,Aib2,3,Leu5xenkephaline. but with a 3.5-fold higher EC50. In comparison, naltrindole was a neutral antagonist while its analogue HS 378 was a partial inverse agonist Emaxsy12.99%..
Inverse agonism by Dmt-Tic analogues and H5 378, a naltrindole analogue
SALVADORI, Severo;BALBONI, Gianfranco;GUERRINI, Remo;
2000
Abstract
The potent d-opioid receptor antagonist H-2X,6- . . L-tyrosine Dmt -1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid Tic-OH exhibited .w35 partial inverse agonism EC50s6.35 nM, Emaxsy18.87% for SxGTPgS binding and H-Dmt–Tic-NH2 was a neutral antagonist no effect up to 30 mM.. In contrast N,NCH3.2-Dmt–Tic-NH2 was a full inverse agonist EC50s2.66 nM, Emaxsy35.95%. similar to ICI 174864 wN,N-diallyl-Tyr1,Aib2,3,Leu5xenkephaline. but with a 3.5-fold higher EC50. In comparison, naltrindole was a neutral antagonist while its analogue HS 378 was a partial inverse agonist Emaxsy12.99%..File in questo prodotto:
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