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zolazepam
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Small Molecules
- Administration
- Intramuscular, Intravenous
01
Overview
Zolazepam is a pyrazolodiazepinone derivative structurally related to benzodiazepines and used primarily as an anesthetic and tranquilizer in veterinary medicine. It is typically administered in combination with tiletamine (an NMDA receptor antagonist) or xylazine (an α2 adrenergic receptor agonist), depending on the clinical need. Zolazepam acts as a positive allosteric modulator of GABA-A receptors, enhancing inhibitory neurotransmission and producing sedation, anxiolysis, muscle relaxation, and anticonvulsant effects. Its onset of action is rapid due to its water solubility and un-ionized state at physiological pH. Zolazepam was developed by Horace A. de Wald and Donald E. Butler for Parke-Davis following detailed analysis of benzodiazepine structures[1][5][6]. In clinical use for animals—including wild species such as gorillas and polar bears—zolazepam/tiletamine combinations are favored over ketamine due to reduced side effects[5].
- Brand names
- TelazolZoletil
- Other names
- Flupyrazaponzolazepam hydrochloridezolazepam HCl
02
Targets
GABRR (GABA-A receptor subunit rho)
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