Drug intelligence / Profile preview

tiletamine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intramuscular, Intravenous
01

Overview

Tiletamine is a dissociative anesthetic agent and a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, chemically related to ketamine and phencyclidine. It is primarily used in veterinary medicine as an injectable anesthetic for cats and dogs, most commonly in combination with zolazepam under the brand names Telazol or Zoletil. Tiletamine produces profound analgesia, cataleptoid anesthesia, and dissociative unconsciousness by selectively interrupting association pathways in the brain before producing somesthetic sensory blockade. Its mechanism of action involves reversible antagonism of NMDA-mediated responses without major effects on normal neuronal membrane properties at low concentrations. Tiletamine has sedative effects in both animals and humans but is mainly approved for veterinary use due to its potential for abuse, toxicity, and hallucinogenic properties[1][2][3][5].

Brand names
TelazolZoletil
Other names
tiletamine hydrochloride
02

Targets

NMDAR (Glutamate receptor ionotropic, NMDA)

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