Imiloxan Explained

Imiloxan is a drug which is used in scientific research. It acts as a selective antagonist for the α_2B adrenergic receptor,^[1] and has been useful for distinguishing the actions of the different α₂ adrenergic subtypes.^{[2] [3]}

Synthesis

The imidazole portion of imiloxan is prepared by the reaction of an imidate with the diethyl acetal of aminoacetaldehyde. N-Alkylation of the imidazole with ethyl iodide gives imiloxan.

Notes and References

1. Michel AD, Loury DN, Whiting RL . Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist . British Journal of Pharmacology . 99 . 3 . 560–4 . March 1990 . 1970500 . 1917331 . 10.1111/j.1476-5381.1990.tb12968.x .
2. Cobos-Puc LE, Villalón CM, Sánchez-López A, Lozano-Cuenca J, Pertz HH, Görnemann T, Centurión D . Pharmacological evidence that alpha2A- and alpha2C-adrenoceptors mediate the inhibition of cardioaccelerator sympathetic outflow in pithed rats . European Journal of Pharmacology . 554 . 2–3 . 205–11 . January 2007 . 17109851 . 10.1016/j.ejphar.2006.09.068 .
3. Romero TR, de Castro Perez A, de Francischi JN, Gama Duarte ID . Probable involvement of alpha(2C)-adrenoceptor subtype and endogenous opioid peptides in the peripheral antinociceptive effect induced by xylazine . European Journal of Pharmacology . 608 . 1–3 . 23–7 . April 2009 . 19236861 . 10.1016/j.ejphar.2009.02.019 . free .