In vivo evaluation of new carfentanil-based radioligands for the mu opiate receptor

2004 ◽  
Vol 31 (3) ◽  
pp. 321-325 ◽  
Author(s):  
Douglas M Jewett ◽  
Michael R Kilbourn
1984 ◽  
Vol 246 (4) ◽  
pp. G386-G392
Author(s):  
R. Fogel ◽  
R. B. Kaplan

Intraluminal administration of naloxone (10(-4) M), a mu-opiate receptor antagonist, or diprenorphine (10(-6) M), an opiate receptor antagonist with high affinity for both delta- and mu-receptors, decreased basal in vivo water and electrolyte absorption in the jejunum and ileum but not the colon of the rat. Diprenorphine (10(-5) M) decreased basal colonic water transport. These changes were not due to a reduction in mucosal Na-K-ATPase activity. Intravenous atropine prevented as well as abolished the changes in water transport due to naloxone. The diprenorphine-induced changes were not altered by atropine. Naloxone and diprenorphine acted by different receptors. Pretreatment with naloxone (10(-4) M) prevented the increase in water transport due to morphine, a mu-agonist, whereas a higher concentration of naloxone (10(-3) M) was required to inhibit the increase due to D-Ala-methionine-enkephalinamide, a delta-receptor agonist. In contrast, diprenorphine (10(-6) M) abolished the absorption caused by morphine and D-Ala-methionine-enkephalinamide. Diprenorphine (3 X 10(-7) M) partially prevented the morphine-induced increase in water absorption.(ABSTRACT TRUNCATED AT 250 WORDS)


1989 ◽  
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H. Saji ◽  
D. Tsutsumi ◽  
J. Konishi ◽  
A. Yokoyama ◽  
Y. Kiso ◽  
...  

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Vincent J Cunningham ◽  
Julian C Matthews ◽  
Eugenii Rabiner ◽  
Steen Jakobsen ◽  
...  

2005 ◽  
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pp. S595-S595 ◽  
Author(s):  
Wynne K Schiffer ◽  
Deborah Pareto-Onghena ◽  
HaiTao Wu ◽  
Kuo-Shyan Lin ◽  
Andrew R Gibbs ◽  
...  

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2010 ◽  
Vol 76 (12) ◽  
Author(s):  
J Bauer ◽  
F Dehm ◽  
A Koeberle ◽  
F Pollastro ◽  
G Appendino ◽  
...  

2008 ◽  
Vol 56 (S 1) ◽  
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S Bleiziffer ◽  
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