Propoxazepam, 7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-one, in the models of nociceptive and neuropathic pain showed significant analgesic activity and also has an anticonvulsant effect, which explains the analgesic component of the pharmacological spectrum. Mechanism of propoxazepam anticonvulsant properties includes GABAergic and glycinergic systems. Antibradykinin and antileukotriene action, dopaminergic system, NMDA, and alpha-1 adrenergic receptors, except the prostaglandin component, are involved in the mechanisms of propoxazepam analgesic effect. Previous pharmacokinetic studies in mice have shown that [214C]Propoxazepam evacuation from stomach (intragastral administration, 10 mg/kg) described as two-phase process (first phase with kel -0,68 h-1, the second of kel = 0,0094 h-1). Total dose quantity, absorbed during experiment, was ~ 80%, with absorption constant of 0,371 ± 0,098 h-1. Similar values of distribution volume (743 ± 195 sm3/kg and 1090 ± 421 g/kg for blood and brain respectively) let suggest intensive mass transfer. LD50 of propoxazepam is greater than 5000 mg/kg and it therefore, belongs to the category V of relatively non-toxic substances according to the GHS. In the acute toxicity study, neither mortality no significant change in the body weight and the relative organ weights were recorded in all treated mice and rats. Propoxazepam did not show the ability to induce gene mutations in the microplate version of the test (Muta-ChromoPlate kit) on the strains Salmonella typhimurium TA 98 and TA 100. The metabolic activation system was also not effective, that is, Propoxazepam is neither a "direct" nor an "indirect" mutagen for Ames strains. The present investigation demonstrates the analgetic and anticonvulsant effects, good bioavailability and safety of propoxazepam suggesting its promising potential for pharmaceutical uses.