Antagonizing effects of YM-14673, a new TRH derivative, on behavioral and electroencephalographic changes in reserpinized animals

Psychopharmacology (Berl). 1988;95(2):162-6. doi: 10.1007/BF00174502.

Abstract

Effects of YM-14673 (N alpha-[[S)-4-oxo-2-azetidinyl)-carbonyl]-L-histidyl-L-prolinamide dihydrate), a new TRH derivative, on reserpine-induced behavioural and electroencephalographic changes were observed in comparison with those of TRH. YM-14673 antagonized reserpine-induced hypothermia and decrease in convulsion threshold in mice. The number of PGO waves recorded from the lateral geniculate body was decreased by administration of YM-14673 in reserpinized cats. The anti-reserpine activity of intravenous YM-14673 was about 8-20 times more potent than that of TRH. In inhibiting reserpine-induced hypothermia, the oral ED2 degrees C relative to IV ED2 degrees C as an indirect indication of absorption rate of the drugs was 15 for both YM-14673 and TRH. These results suggest that YM-14673 possesses more potent facilitatory effects on the central monoamine systems than TRH.

MeSH terms

  • Animals
  • Azetidines / pharmacology*
  • Azetines / pharmacology*
  • Behavior, Animal / drug effects*
  • Body Temperature / drug effects
  • Cats
  • Dipeptides / pharmacology*
  • Electroencephalography*
  • Female
  • Male
  • Mice
  • Mice, Inbred ICR
  • Reserpine / antagonists & inhibitors*
  • Seizures / chemically induced
  • Thyrotropin-Releasing Hormone / analogs & derivatives*
  • Thyrotropin-Releasing Hormone / pharmacology

Substances

  • Azetidines
  • Azetines
  • Dipeptides
  • Thyrotropin-Releasing Hormone
  • azetirelin
  • Reserpine