Cirazoline Explained

Cirazoline is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors,[1] and a nonselective antagonist to the α2 adrenergic receptor.[2] It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.[2]

Cirazoline has also been shown to decrease food intake in rats, purportedly through activation of α1 adrenoceptors in the paraventricular nucleus in the hypothalamus of the brain.[3] Administration of cirazoline also seemed to present impairment in the spatial memory of monkeys through the activation of the same receptors that showed decreased food intake in rats.[4] [5] However, in preliminary studies, through stimulation of α2 adrenoceptors, working memory is comparatively improved.

Notes and References

  1. Horie, K . Obika, K . Foglar, R. . Selectivity of the imidazoline α-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned α1-adrenoceptor subtypes . British Journal of Pharmacology . 1995 . 116 . 1 . 1611–8 . 8564227 . 10.1111/j.1476-5381.1995.tb16381.x . 1908909.
  2. Ruffolo, R. R. Jr. . Waddell, J. E. . Receptor interactions of imidazolines. IX. Cirazoline is an α1 adrenergic agonist and an α2 adrenergic antagonist . Journal of Pharmacology and Experimental Therapeutics . 1982 . 222 . 1 . 29–36 . 6123592 .
  3. Davies, B. T. . Wellman, P. J. . 1992 . Effects on ingestive behavior in rats of the α1-adrenoceptor agonist cirazoline . European Journal of Pharmacology . 210 . 1 . 11–16 . 10.1016/0014-2999(92)90645-K . 1350985 .
  4. Arnsten . A.F.T. . Jentsch . J.D. . September 1997 . The Alpha-1 Adrenergic Agonist, Cirazoline, Impairs Spatial Working Memory Performance in Aged Monkeys . Pharmacology Biochemistry and Behavior . 58 . 1 . 55–59 . 10.1016/s0091-3057(96)00477-7 . 9264070 . 20663570 . 0091-3057. free .
  5. Imbery, Irdmusa, Speidell, Streer, Griffin . Ted E., Mitra S., Andrew P., Mark S., John D. . 15 December 2007 . The effects of Cirazoline, an alpha-1 adrenoreceptor agonist, on the firing rates of thermally classified anterior hypothalamic neurons in rat brain slices . Brain Research . 1193 . 93–101 . 10.1016/j.brainres.2007.12.016 . 18184607 . 2268753 .

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