Analgesic actions and local anesthetic activity of 3-acetylaconitine hydrobromide
Abstract
3-Acetylaconitine was first isolated from the root of Aconitum flavum and A. pendulum. The analgesic and local anesthetic activity of 3-acetylaconitine hydrobromide were studied in this paper.
The sc median analgesic dose (ED50) in mice were 0.21 and 0.13 mg/kg, respectively, with the hot plate and stretching method induced by ip 0.7% acetic acid. Its analgesic action was stronger than that of aconitine. 3-Acetylaconitine possessed a weak corneal anesthetic activity. Its local anesthetic activities on sciatic nerve block in mice and intracutaneous wheal test in guinea pig were found to be 92 and 53 times, respectively, as active as cocaine. The sc LD50 of 3-acetylaconitine was 1.4 mg/kg in mice, its acute toxicity was lower than that of aconitine. So 3-acetylaconitine exhibited a higher therapeutic index than aconitine.
Keywords:
The sc median analgesic dose (ED50) in mice were 0.21 and 0.13 mg/kg, respectively, with the hot plate and stretching method induced by ip 0.7% acetic acid. Its analgesic action was stronger than that of aconitine. 3-Acetylaconitine possessed a weak corneal anesthetic activity. Its local anesthetic activities on sciatic nerve block in mice and intracutaneous wheal test in guinea pig were found to be 92 and 53 times, respectively, as active as cocaine. The sc LD50 of 3-acetylaconitine was 1.4 mg/kg in mice, its acute toxicity was lower than that of aconitine. So 3-acetylaconitine exhibited a higher therapeutic index than aconitine.