Effects of the nicotinic agonist varenicline, nicotinic antagonist r-bPiDI, and DAT inhibitor (R)-modafinil on co-use of ethanol and nicotine in female P rats

Psychopharmacology (Berl). 2018 May;235(5):1439-1453. doi: 10.1007/s00213-018-4853-4. Epub 2018 Feb 18.

Abstract

Rationale: Co-users of alcohol and nicotine are the largest group of polysubstance users worldwide. Commonalities in mechanisms of action for ethanol (EtOH) and nicotine proposes the possibility of developing a single pharmacotherapeutic to treat co-use.

Objectives: Toward developing a preclinical model of co-use, female alcohol-preferring (P) rats were trained for voluntary EtOH drinking and i.v. nicotine self-administration in three phases: (1) EtOH alone (0 vs. 15%, two-bottle choice), (2) nicotine alone (0.03 mg/kg/infusion, active vs. inactive lever), and (3) concurrent access to both EtOH and nicotine. Using this model, we examined the effects of (1) varenicline, a nicotinic acetylcholine receptor (nAChR) partial agonist with high affinity for the α4β2* subtype; (2) r-bPiDI, a subtype-selective antagonist at α6β2* nAChRs; and (3) (R)-modafinil, an atypical inhibitor of the dopamine transporter (DAT).

Results: In phases 1 and 2, pharmacologically relevant intake of EtOH and nicotine was achieved. In the concurrent access phase (phase 3), EtOH consumption decreased while nicotine intake increased relative to phases 1 and 2. For drug pretreatments, in the EtOH access phase (phase 1), (R)-modafinil (100 mg/kg) decreased EtOH consumption, with no effect on water consumption. In the concurrent access phase, varenicline (3 mg/kg), r-bPiDI (20 mg/kg), and (R)-modafinil (100 mg/kg) decreased nicotine self-administration but did not alter EtOH consumption, water consumption, or inactive lever pressing.

Conclusions: These results indicate that therapeutics which may be useful for smoking cessation via selective inhibition of α4β2* or α6β2* nAChRs, or DAT inhibition, may not be sufficient to treat EtOH and nicotine co-use.

Keywords: (R)-modafinil; Alcohol; Co-use; Ethanol; Nicotine; R-bPiDI; Varenicline.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alcohol Drinking / drug therapy
  • Alcohol Drinking / psychology
  • Animals
  • Dopamine Plasma Membrane Transport Proteins / antagonists & inhibitors*
  • Dopamine Plasma Membrane Transport Proteins / physiology
  • Dose-Response Relationship, Drug
  • Ethanol / administration & dosage*
  • Female
  • Modafinil / pharmacology*
  • Modafinil / therapeutic use
  • Nicotine / administration & dosage*
  • Nicotinic Agonists / pharmacology*
  • Nicotinic Agonists / therapeutic use
  • Nicotinic Antagonists / pharmacology*
  • Nicotinic Antagonists / therapeutic use
  • Rats
  • Receptors, Nicotinic / physiology
  • Self Administration
  • Smoking Cessation / methods
  • Varenicline / pharmacology*
  • Varenicline / therapeutic use

Substances

  • Dopamine Plasma Membrane Transport Proteins
  • Nicotinic Agonists
  • Nicotinic Antagonists
  • Receptors, Nicotinic
  • Ethanol
  • Nicotine
  • Modafinil
  • Varenicline