Description
Piperoxan is an α
2-adrenergic receptor (α
2-AR) antagonist (K
is = 5.4, 2, and 1.3 nM for α
2A-, α
2B-, and α
2C-ARs, respectively) and a first generation histamine receptor antagonist. It reverses decreases in systolic blood pressure induced by clonidine in spontaneously hypertensive rats when administered at a dose of 10 mg/kg.
Uses
Piperoxan (Benodaine) hydrochloride is an α2 adrenoceptor antagonist. Piperoxan hydrochloride is the first-generation antihistamine.
Safety Profile
Poison by
intraperitoneal and intravenous routes.
Moderately toxic by ingestion and
subcutaneous routes. Experimental
reproductive effects. When heated to
decomposition it emits very toxic fumes of
NO, and HCl.
References
[1] Viemari JC, et al. Nasal trigeminal inputs release the A5 inhibition received by the respiratory rhythm generator of the mouse neonate. J Neurophysiol. 2004 Feb;91(2):746-58. DOI:
10.1152/jn.01153.2002[2] Bentley GA, et al. The antinociceptive action of some beta-adrenoceptor agonists in mice. Br J Pharmacol. 1986 Jul;88(3):515-21. DOI:
10.1111/j.1476-5381.1986.tb10231.x