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Tripelennamine interactions with the psychotomimetic sigma agonist N-allylnormetazocine.

D B Vaupel

Pharmacology, biochemistry, and behavior July 1989 DOI: 10.1016/0091-3057(89)90414-0 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics Animal experimental study Peer reviewed
Population Chronic spinal dogs
Interventions Tripelennamine N-allylnormetazocine (NANM)
Dose Tripelennamine 1.25 mg/kg IV; NANM 1.65 mg/kg IV
Key findings NANM produced antinociception, mydriasis, tachycardia, hyperthermia, and canine delirium, while tripelennamine produced antinociception, mydriasis, and tachycardia without behavioral effects. The drugs' combined effects were additive except for heart rate, and tripelennamine did not antagonize NANM's physiological or delirium effects. The authors state these findings are inconsistent with the hypothesis that tripelennamine antagonizes NANM-like psychotomimetic effects of pentazocine to make pentazocine-tripelennamine combinations more desirable as a heroin substitute.

Abstract

The pharmacological effects of individual and combined intravenous doses of the antihistamine tripelennamine and the psychotomimetic sigma benzomorphan opioid derivative, N-allylnormetazocine (NANM), on nociceptive reflexes, autonomic parameters and behavior were assessed in the chronic spinal dog. NANM (1.65 mg/kg, IV) produced antinociception, mydriasis, tachycardia, hyperthermia and behavioral signs of canine delirium. Tripelennamine (1.25 mg/kg, IV) produced antinociception, mydriasis and tachycardia without affecting behavior. The combined effects of the two drugs were additive except for heart rate. However, tripelennamine did not antagonize any of the physiological effects or the signs of canine delirium produced by NANM. The findings are inconsistent with the hypothesis that tripelennamine antagonizes the psychotomimetic NANM-like effects of pentazocine to make pentazocine-tripelennamine combinations (T's and Blues) more desirable as a heroin substitute.