Opioid agonist and antagonist behavioural effects of buprenorphine

The Effects of Nalbuphine and Butorphanol Treatment on Cocaine and Food Self-Administration by Rhesus Monkeys

“…Acute buprenorphine administration usu ally reduces food self-administration (Dykstra 1983;Leander 1983;Lukas et al 1986;Mello et al 1985) but tolerance develops during chronic administration (Lu kas et al 1988; Mello et al 1981Mello et al , 1985Mello et al , 1992. antagonist actions under some conditions.…”

The effects of chronic buprenorphine on intake of heroin and cocaine in rats and its effects on nucleus accumbens dopamine levels during self-administration

“…Regardless of this high dose of buprenorphine, total heroin intake was not significantly suppressed under any of the conditions, whereas the DA response in the NAc to heroin infusions was totally absent; thus, there was a dissociation between the effectiveness of heroin as a reinforcer and the magnitude of the DA response to the infusion in the NAc. Not surprisingly, buprenorphine blocks the subjective and behavioral effects of other mu receptor agonists in a variety of species in various tests (Bickel et al 1988;Filibeck et al 1981;Leander 1983) likely due to its high affinity for and slow dissociation from the mu opioid receptor. Furthermore, it is known that antagonism of opioid receptors in the NAc (Vaccarino et al 1985) or VTA (Britt and Wise 1983), which would effectively reduce the "dose" of heroin, results in an (right panel, rats #1, 3, 4, 6, 7, and 9; gray bars).…”

Behavioral pharmacology of buprenorphine, with a focus on preclinical models of reward and addiction

“…Most commonly, in studies addressing the stimulus properties of opiates, morphine was used as a training drug (in some cases, fentanyl, etorphine or codeine was used as a training drug), and with few exceptions (see below) a full substitution of buprenorphine for the µ-agonist cue was obtained in rats (Colpaert 1978;Shannon et al 1984;Hoffmeister 1988;Negus et al 1990;Young et al 1991a;Paronis and Holtzman 1994;Walker et al 1994;Craft et al 1999;Morgan et al 1999), pigeons (Leander 1983;France et al 1984;France and Woods 1985;Picker and Dykstra 1989;Picker and Cook 1997;Morgan and Picker 1998), monkeys (Schaefer and Holtzman 1981;Young et al 1984;Negus et al 1991) and also humans (Jasinski et al 1978;Preston et al 1992;Preston and Bigelow 1994). A full substitution between buprenorphine and the mixedopioid agonist/antagonists dezocine (pigeon) (Picker 1997) and nalbuphine (rat) (Walker and Young 1993) was also found.…”

“…Due to its partial agonist properties with limited intrinsic efficacy, buprenorphine can behave as a pure µ agonist, yet it can also antagonize the actions of morphine and other high-efficacy µ agonists (Leander 1983;Bickel et al 1988b), i.e. it can have either µ-agonistic or µ-antagonistic effects, depending on the particular conditions under which it is evaluated.…”