Reversal of electrophysiological and behavioral deficits mediated by 5-HT7 receptor upregulation following LP-211 treatment in an autistic-like rat model induced by prenatal valproic acid exposure

Neuropharmacology. 2024 Oct 1:257:110057. doi: 10.1016/j.neuropharm.2024.110057. Epub 2024 Jul 2.

Abstract

Autism spectrum disorder (ASD) is a neurodevelopmental disorder characterized by alterations and imbalances in multiple brain neurochemical systems, particularly the serotonergic neurotransmission. This includes changes in serotonin (5-HT) levels, aberrations in 5-HT transporter activity, and decreased synthesis and expression of 5-HT receptors (5-HT7Rs). The exact role of the brain 5-HT system in the development of ASD remains unclear, with conflicting evidence on its involvement. Recently, we have reported research has shown a significant decrease in serotonergic neurons originating from the raphe nuclei and projecting to the CA1 region of the dorsal hippocampus in autistic-like rats. Additionally, we have shown that chronic activation of 5-HT7Rs reverses the effects of autism induction on synaptic plasticity. However, the functional significance of 5-HT7Rs at the cellular level is still not fully understood. This study presents new evidence indicating an upregulation of 5-HT7R in the CA1 subregion of the hippocampus following the induction of autism. The present account also demonstrates that activation of 5-HT7R with its agonist LP-211 can reverse electrophysiological abnormalities in hippocampal pyramidal neurons in a rat model of autism induced by prenatal exposure to VPA. Additionally, in vivo administration of LP-211 resulted in improvements in motor coordination, novel object recognition, and a reduction in stereotypic behaviors in autistic-like offspring. The findings suggest that dysregulated expression of 5-HT7Rs may play a role in the pathophysiology of ASD, and that agonists like LP-211 could potentially be explored as a pharmacological treatment for autism spectrum disorder.

Keywords: Autism; CA1 pyramidal neurons; Neuronal excitability; Upregulation of 5-HT7Rs; Valproic acid; Whole-cell patch-clamp.

MeSH terms

  • Animals
  • Autism Spectrum Disorder / drug therapy
  • Autism Spectrum Disorder / metabolism
  • Autistic Disorder / drug therapy
  • Autistic Disorder / metabolism
  • CA1 Region, Hippocampal / drug effects
  • CA1 Region, Hippocampal / metabolism
  • Disease Models, Animal*
  • Female
  • Male
  • Piperazines / pharmacology
  • Pregnancy
  • Prenatal Exposure Delayed Effects* / chemically induced
  • Prenatal Exposure Delayed Effects* / metabolism
  • Rats
  • Rats, Wistar
  • Receptors, Serotonin* / metabolism
  • Up-Regulation* / drug effects
  • Valproic Acid* / pharmacology

Substances

  • Receptors, Serotonin
  • Valproic Acid
  • N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide
  • serotonin 7 receptor
  • Piperazines
  • 5-HT(7) receptor, rat