Dose-dependent attenuation of heroin self-administration with lobeline.

Behavioural studies have yielded results that show lobeline has the ability to attenuate d-methamphetamine self-administration. Further in vivo and in vitro studies have demonstrated a blockade of mu-opioid receptors with lobeline. The present investigation examined the ability of lobeline to attenuate heroin intravenous (i.v.) self-administration when administered prior to testing. Male Sprague-Dawley rats were surgically implanted with jugular catheters and trained to lever press for i.v. heroin infusions (18 microg/kg) under a fixed ratio-2 schedule wherein two active lever presses resulted in heroin delivery. Rats then were tested for heroin self-administration after pretreatment with subcutaneous lobeline injections (0.3, 1.0, or 3.0 mg/kg, 15 min prior to testing sessions). At doses of 1.0 and 3.0 mg/kg, lobeline attenuated self-administration of heroin. The results suggest a potential for lobeline to be used in pharmacotherapy for opioid abuse.