Inhibition by adenosine analogs of opiate withdrawal effects.
The stable derivatives of adenosine, 2-chloroadenosine and N6-cyclohexyladenosine, with high affinity for the A1 (Ri) adenosine receptor, suppress the naloxone-precipitated withdrawal contracture of the opiate-dependent guinea-pig ileum in vitro. These adenosine derivatives also inhibit naloxone-precipitated jumping, diarrhea and weight-loss in morphine-dependent mice. This effect was not due to sedation, since (i) 2-chloroadenosine was effective at a non-sedative dose and (ii) sedative doses of chlordiazepoxide were ineffective.
D015762:2-Chloroadenosine; D000241:Adenosine / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002707:Chlordiazepoxide / Q000494:pharmacology; D006168:Guinea Pigs; D006801:Humans; D007082:Ileum / Q000294:innervation; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009021:Morphine Dependence / Q000503:physiopathology*; D009022:Morphine Derivatives / Q000009:adverse effects*; D009119:Muscle Contraction / Q000187:drug effects; D009197:Myenteric Plexus / Q000187:drug effects; D009270:Naloxone / Q000494:pharmacology; D011956:Receptors, Cell Surface / Q000187:drug effects; D011983:Receptors, Purinergic; D013375:Substance Withdrawal Syndrome / Q000517:prevention & control*
D009022:Morphine Derivatives; D011956:Receptors, Cell Surface; D011983:Receptors, Purinergic; D015762:2-Chloroadenosine; C027513:N(6)-cyclohexyladenosine; D009270:Naloxone; D002707:Chlordiazepoxide; D000241:Adenosine; C010616:normorphine