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  • Cardiovascular stimulant actions of bupropion in comparison to cocaine in the rat.

Cardiovascular stimulant actions of bupropion in comparison to cocaine in the rat.

European journal of pharmacology (2014-04-24)
Lyndsey M Killian, James R Docherty
ABSTRACT

Stimulants are banned in competition by the World Anti-Doping Agency, except for a small number of therapeutic agents subject to monitoring, including bupropion. We have examined the potency of bupropion in comparison with two agents banned in competition, adrafinil and modafinil, and with cocaine and desipramine as blockers of the noradrenaline re-uptake transporter in peripheral tissues of the rat. For studies in vivo, the pressor response to noradrenaline in the anaesthetized rat was studied. Cocaine, desipramine and bupropion at doses of 0.1, 0.3 and 1mg/kg, respectively, significantly increased the pressor response to noradrenaline. Overall, cocaine and desipramine were approximately 2-5 times more potent than bupropion in vivo in the rat. Adrafinil and modafinil (both 3mg/kg) did not significantly affect the pressor response. Bupropion was chosen for further study. In 1Hz paced rat right ventricular strips, bupropion (30μM) significantly increased the potency of noradrenaline at increasing the force of contraction. In rat vas deferens, bupropion and cocaine produced concentration-dependent increases in the contractile response to nerve stimulation, and cocaine was 11 times more potent than bupropion. Since bupropion is used clinically in doses of up to 300mg, it is likely that bupropion has actions at the noradrenaline transporter, and thus cardiovascular stimulant actions, in clinical doses. This may explain findings of increased exercise performance with bupropion.

MATERIALS
Product Number
Brand
Product Description

Supelco
Nifedipine, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Desipramine hydrochloride solution, 1.0 mg/mL in methanol (as free base), ampule of 1 mL, certified reference material, Cerilliant®
Supelco
Cocaine hydrochloride solution, 1.0 mg/mL in methanol, analytical standard, for drug analysis
Sigma-Aldrich
Methoxamine hydrochloride
Sigma-Aldrich
Cocaine hydrochloride
Sigma-Aldrich
Nifedipine, ≥98% (HPLC), powder
USP
Nifedipine, United States Pharmacopeia (USP) Reference Standard
Nifedipine, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
Desipramine hydrochloride, ≥98% (TLC), powder
USP
Desipramine hydrochloride, United States Pharmacopeia (USP) Reference Standard
Desipramine hydrochloride, European Pharmacopoeia (EP) Reference Standard