Isoxsuprine-d
6 is intended for use as an internal standard for the quantification of isoxsuprine by GC- or LC-MS. Isoxsuprine is an adrenergic receptor modulator that has α-adrenergic receptor (α-AR) antagonist and β-AR agonist properties.
1,2 It induces vasodilation of isolated equine common digital artery strips precontracted with norepinephrine, indicating an α-AR effect, and induces relaxation of isolated fowl cecum, an effect that can be blocked by the β-AR antagonist propranolol .
2,3 Isoxsuprine has antinociceptive effects in an acetic acid writhing test in mice.
4 It also inhibits oxytocin-induced contractions in isolated rat uterus (IC
50 = 9.15 μM).
5 It delays labor onset in rats by 31.63 hours when administered at a dose of 10 mg/kg per day on days 13 to 21 of gestation but increases heart rate with increasing concentration.
Isoxsuprine-d6 (hydrochloride) is the deuterium labeled Isoxsuprine hydrochloride. Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
1. Cook, P., and James, I. Cerebral vasodilators (second of two parts) N. Engl. J. Med. 305(26),1560-1564(1981).
2. Belloli, C., Carcano, R., Arioli, F., et al. Affinity of isoxsuprine for adrenoreceptors in equine digital artery and implications for vasodilatory action Equine Vet. J. 32(2),119-124(2000).
3. Ekert, R.S., and Macallister, C.G. Isoxsuprine hydrochloride in the horse: A review J. Vet. Pharmacol. Ther. 25(2),81-87(2002).
4. Bentley, G.A., and Starr, J. The antinociceptive action of some β-adrenoceptor agonists in mice Br. J. Pharmacol. 88(3),515-521(1988).
5. Viswanathan, C.L., Kodgule, M.M., and Chaudhari, A.S. Design, synthesis and evaluation of racemic 1-(4-hydroxyphenyl)-2-[3-(substituted phenoxy)-2-hydroxy-1-propyl]amino-1-propanol hydrochlorides as novel uterine relaxants Bioorg. Med. Chem. Lett. 15(15),3532-3535(2005).
