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  • Title: Effect of peptides on the development of tolerance to buprenorphine, a mixed opiate agonist-antagonist analgesic.
    Author: Bhargava HN.
    Journal: Eur J Pharmacol; 1982 Apr 08; 79(1-2):117-23. PubMed ID: 7084303.
    Abstract:
    The subcutaneous administration of buprenorphine to male Sprague-Dawley rats produced a dose-dependent analgesia and hyperthermia in a dose range of 0.25-2 mg/kg. The subcutaneous administration of buprenorphine (0.5 mg/kg) twice a day for 4 days resulted in the development of tolerance to its analgesic and hyperthermic actions. Daily administration of melanotropin release inhibiting factor (Pro-Leu-Gly-NH2) or cyclo (Leu-Gly) (2 mg/kg s.c.) for 4 days, inhibited the development of tolerance to buprenorphine, as evidenced by greater analgesic and hyperthermic responses to buprenorphine in peptide-treated than in vehicle-treated buprenorphine-tolerant rats. The repeated injections of peptides did not alter the analgesic or the hyperthermic response to buprenorphine in non-tolerant rats. These studies suggest the possible role of hypothalamic peptides in blocking the development of tolerance to the pharmacological effects of buprenorphine, a potent analgesic agent.
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