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BUPRENORPHINE AND GASTROINTESTINAL TRANSIT IN RATS: EFFECT OF NALOXONE ON THE BIPHASIC DOSE‐RESPONSE CURVE
Author(s) -
Cowan Alan
Publication year - 1992
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.1992.tb00396.x
Subject(s) - buprenorphine , (+) naloxone , pharmacology , ed50 , medicine , chemistry , opioid , anesthesia , receptor
SUMMARY 1. Buprenorphine (0.01–10 mg/kg, subcutaneous [s.c.]) slowed the passage of a charcoal meal along the gastrointestinal tract in rats. The dose‐response relationship was U‐shaped. 2. When rats were pretreated with naloxone (0.30 mg/kg, s.c), both the descending and ascending components of the buprenorphine dose‐response curve were displaced to the right. 3. Buprenorphine‐induced delay of transit was maximal at a dose of 0.10 mg/kg. In rats pretreated with naloxone, a 30‐fold higher dose of buprenorphine was required for a comparable peak effect. 4. Moderate‐high doses of buprenorphine may be acting on a functionally related binding site which non‐competitively inhibits the usual buprenorphine‐μ opioid receptor interaction.