Antazoline HCl | Antihistamine and neuroprotective

Antazoline HCl chemical structure

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Antazoline (2508-72-7) displays neuroprotective effects against hypoxia-induced death in neuronal cultures, the mechanism of action being inhibition of NMDA currents (IC50=4 µM).1  It induces concentration-dependent stimulation of insulin secretion in rat pancreas which is mediated via imidazoline I1 receptors.2  It also acts as a histamine H1 receptor antagonist (Ki=38.4 nM, human recombinant H1 receptor)3 and was found to be a highly effective antiarrhythmic agent4.

References/Citations:

  1. Mihaud et al. (2000), Imidazoline-induced neuroprotective effects result from blockade of NMDA receptor channels in neuronal cultures; Neuropharmacology 39 2244
  2. Berdeu et al. (1995), Evidence for two different imidazoline sites on pancreatic B cells and vascular bed in rat; Eur. J. Pharmacol. 275 91
  3. Yanni et al. (1999), Inhibition of histamine-induced human conjunctival epithelial cell responses by ocular allergy drugs; Arch. Ophthamol. 117 643
  4. Frommeyer et al. (2017), Effective suppression of atrial fibrillation by the antihistaminic agent antazoline: First experimental insights into a novel antiarrhythmic agent; Cardiovasc. Ther. 35 e12244
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Antazoline (2508-72-7) displays neuroprotective effects against hypoxia-induced death in neuronal cultures, the mechanism of action being inhibition of NMDA currents (IC50=4 µM).1  It induces concentration-dependent stimulation of insulin secretion in rat pancreas which is mediated via imidazoline I1 receptors.2  It also acts as a histamine H1 receptor antagonist (Ki=38.4 nM, human recombinant H1 receptor)3 and was found to be a highly effective antiarrhythmic agent4.

References/Citations:

  1. Mihaud et al. (2000), Imidazoline-induced neuroprotective effects result from blockade of NMDA receptor channels in neuronal cultures; Neuropharmacology 39 2244
  2. Berdeu et al. (1995), Evidence for two different imidazoline sites on pancreatic B cells and vascular bed in rat; Eur. J. Pharmacol. 275 91
  3. Yanni et al. (1999), Inhibition of histamine-induced human conjunctival epithelial cell responses by ocular allergy drugs; Arch. Ophthamol. 117 643
  4. Frommeyer et al. (2017), Effective suppression of atrial fibrillation by the antihistaminic agent antazoline: First experimental insights into a novel antiarrhythmic agent; Cardiovasc. Ther. 35 e12244