Tacr1 gene variation and neurokinin 1 receptor expression is associated with antagonist efficacy in genetically selected alcohol-preferring rats

Biol Psychiatry. 2013 Apr 15;73(8):774-81. doi: 10.1016/j.biopsych.2012.12.027. Epub 2013 Feb 16.

Abstract

Background: Genetic deletion or antagonism of the neurokinin 1 receptor (NK1R) decreases alcohol intake, alcohol reward, and stress-induced alcohol relapse in rodents, while TACR1 variation is associated with alcoholism in humans.

Methods: We used L822429, a specific antagonist with high affinity for the rat NK1R, and examined whether sensitivity to NK1R blockade is altered in alcohol-preferring (P) rats. Operant alcohol self-administration and progressive ratio responding were analyzed in P-rats and their founder Wistar line. We also analyzed Tacr1 expression and binding and sequenced the Tacr1 promoter from both lines.

Results: Systemic L822429 decreased alcohol self-administration in P-rats but did not affect the lower rates of alcohol self-administration in Wistar rats. Tacr1 expression was elevated in the prefrontal cortex and the amygdala of P-rats. In central amygdala, elevated Tacr1 expression was accompanied by elevated NK1R binding. Central amygdala (but not prefrontal cortex) infusion of L822429 replicated the systemic antagonist effects on alcohol self-administration in P-rats. All P-rats, but only 18% of their founder Wistar population, were CC homozygous for a-1372G/C single nucleotide polymorphism. In silico analysis indicated that the Tacr1-1372 genotype could modulate binding of the transcription factors GATA-2 and E2F-1. Electromobility shift and luciferase reporter assays suggested that the-1372C allele confers increased transcription factor binding and transcription.

Conclusions: Genetic variation at the Tacr1 locus may contribute to elevated rates of alcohol self-administration, while at the same time increasing sensitivity to NK1R antagonist treatment.

Publication types

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

MeSH terms

  • Alcohol Drinking / genetics*
  • Amygdala / drug effects
  • Amygdala / metabolism
  • Animals
  • Conditioning, Operant / drug effects
  • Conditioning, Operant / physiology
  • E2F1 Transcription Factor / metabolism
  • Ethanol / administration & dosage
  • Ethanol / pharmacology*
  • GATA Transcription Factors / metabolism
  • Male
  • Microinjections
  • Neurokinin-1 Receptor Antagonists / administration & dosage
  • Neurokinin-1 Receptor Antagonists / pharmacology*
  • Piperidines / administration & dosage
  • Piperidines / pharmacology
  • Polymorphism, Single Nucleotide / genetics*
  • Prefrontal Cortex / drug effects
  • Prefrontal Cortex / metabolism
  • Rats
  • Receptors, Neurokinin-1 / genetics
  • Receptors, Neurokinin-1 / metabolism*
  • Self Administration

Substances

  • E2F1 Transcription Factor
  • E2f1 protein, rat
  • GATA Transcription Factors
  • N-((2-cyclopropoxy-5-(5-trifluomethyl)tetrazol-1-yl)benzyl)-2-phenylpiperidin-3-amine
  • Neurokinin-1 Receptor Antagonists
  • Piperidines
  • Receptors, Neurokinin-1
  • Ethanol