Protein Information

Name alpha 2 adrenoreceptor
Synonyms Alpha 2A Adrenoceptor; ZNF32; ADRA2; ADRA2A; ADRA2R; ADRAR; ALPHA2AAR; Alpha 2A adrenergic receptor…

Compound Information

Name amitraz
CAS

Reference List

PubMed Abstract RScore(About this table)
3000030 Moser VC, MacPhail RC: Yohimbine attenuates the delayed lethality induced in mice by amitraz, a formamidine pesticide. Toxicol Lett. 1985 Nov;28(2-3):99-104.

These data suggest that an alpha 2-adrenergic mechanism is involved in the delayed lethality produced by amitraz.
81(1,1,1,1) Details
3758001 Roberts MC, Argenzio A: Effects of amitraz, several opiate derivatives and anticholinergic agents on intestinal transit in ponies. Equine Vet J. 1986 Jul;18(4):256-60.

The results suggest potential clinical applications in horses for loperamide in diarrhoea therapy, for alpha 2 adrenergic antagonists in obstruction and ileus and, possibly, of amitraz-like agents in reducing fluid losses in diarrhoea.
37(0,1,2,2) Details
15516314 Lehner AF, Hughes CG, Karpiesiuk W, Harkins JD, Dirikolu L, Bosken J, Camargo F, Boyles J, Troppmann A, Woods WE, Tobin T: Development of a method for the detection and confirmation of the alpha-2 agonist amitraz and its major metabolite in horse urine. J Anal Toxicol. 2004 Oct;28(7):553-62.

Amitraz (N'-(2,4-dimethylphenyl)-N-[[(2,4-dimethylphenyl) imino] methyl]-N-methyl-me thanimidamide) is an alpha-2 adrenergic agonist used in veterinary medicine primarily as a scabicide- or acaricide-type insecticide.
32(0,1,1,2) Details
15822764 Gursoy S, Kunt N, Kaygusuz K, Kafali H: Intravenous amitraz poisoning. Clin Toxicol. 2005;43(2):113-6.

Amitraz inhibits monoamine oxidase and prostaglandin synthesis and is an alpha-2 adrenergic agonist.
31(0,1,1,1) Details
1675967 Pass MA, Mogg TD: Effect of amitraz and its metabolites on intestinal motility. Comp Biochem Physiol C. 1991;99(1-2):169-72.

The results suggest that despite the significant antihistamine activity of amitraz and BTS27271 in vitro, it is probably the alpha-2-adrenergic agonist activity that is the most important in causing large intestinal stasis in vivo.
31(0,1,1,1) Details
3012823 Hsu WH, Lu ZX, Hembrough FB: Effect of amitraz on heart rate and aortic blood pressure in conscious dogs: influence of atropine, prazosin, tolazoline, and yohimbine. Toxicol Appl Pharmacol. 1986 Jun 30;84(2):418-22.

Yohimbine, an alpha 2-adrenoreceptor antagonist, given iv at 0.1 mg/kg, prevented hypertension, bradycardia, and sinus arrhythmia induced by amitraz.
31(0,1,1,1) Details
2157035 Cullen LK, Reynoldson JA: Central and peripheral alpha-adrenoceptor actions of amitraz in the dog. J Vet Pharmacol Ther. 1990 Mar;13(1):86-92.
6(0,0,1,1) Details
2884938 Hsu WH, Shaw RN, Schaffer DD, Crump MH, Greer MH: Further evidence to support the alpha 2-adrenergic nature of amitraz-induced decrease in intestinal motility. Arch Int Pharmacodyn Ther. 1987 Mar;286(1):145-51.
6(0,0,1,1) Details
2508150 Gilbert ME, Mack CM: Enhanced susceptibility to kindling by chlordimeform may be mediated by a local anesthetic action. Psychopharmacology. 1989;99(2):163-7.

The formamidine pesticides amitraz and chlordimeform have recently been shown to be potent proconvulsants (Gilbert 1988).
Two main neuroactive properties have been identified as mediators of formamidine neurotoxicity, alpha-2 adrenergic agonism and local anesthetic actions.
2(0,0,0,2) Details
2163971 Wu D, Costa LG, Murphy SD: [The effect of pesticides-CDM and AMZ on inhibition of the binding of 3H-clonidine to alpha 2-adrenoreceptor in rat forebrain tissue]. Hua Xi Yi Ke Da Xue Xue Bao. 1990 Mar;21(1):17-21.

Chlordimeform (CDM) and Amitraz (AMZ) are two formamidine pesticides.
2(0,0,0,2) Details
9363478 Jorens PG, Zandijk E, Belmans L, Schepens PJ, Bossaert LL: An unusual poisoning with the unusual pesticide amitraz. . Hum Exp Toxicol. 1997 Oct;16(10):600-1.

We report on a case of human poisoning with amitraz with typical signs of alpha 2-adrenoreceptor stimulation.
7(0,0,1,2) Details
3211100 Gilbert ME: Formamidine pesticides enhance susceptibility to kindled seizures in amygdala and hippocampus of the rat. Neurotoxicol Teratol. 1988 May-Jun;10(3):221-7.

Electrical kindling of the amygdala and hippocampus was used to evaluate the effects of two formamidines, chlordimeform (CDF) and amitraz (AMZ), upon seizures susceptibility in the rat.
The alpha-2 adrenergic agonist and/or local anesthetic-like properties of these compounds may be responsible for these seizure enhancing effects.
1(0,0,0,1) Details
2385843 Schaffer DD, Hsu WH, Hopper DL: The effects of yohimbine and four other antagonists on amitraz-induced depression of shuttle avoidance responses in dogs. Toxicol Appl Pharmacol. 1990 Jul;104(3):543-7.

0(0,0,0,0) Details
6326347 Hsu WH, Kakuk TJ: Effect of amitraz and chlordimeform on heart rate and pupil diameter in rats: mediated by alpha 2-adrenoreceptors. Toxicol Appl Pharmacol. 1984 May;73(3):411-5.

Amitraz-induced mydriasis and bradycardia were blocked by antagonists with alpha 2-adrenoreceptor blocking activity: yohimbine and phentolamine (2.5 mg/kg each, iv).
112(1,2,2,2) Details
4075998 Hsu WH, McNeel SV: Amitraz-induced prolongation of gastrointestinal transit and bradycardia in dogs and their antagonism by yohimbine: preliminary study. Drug Chem Toxicol. 1985;8(4):239-53.

Yohimbine, an alpha 2-adrenergic blocking agent, given IV 20 minutes after amitraz administration, at a dosage of 0.1 mg/kg, reversed both the gastrointestinal and bradycardic effects of amitraz.
81(1,1,1,1) Details
11312645 Altobelli D, Martire M, Maurizi S, Preziosi P: Interaction of formamidine pesticides with the presynaptic alpha (2)-adrenoceptor regulating. Toxicol Appl Pharmacol. 2001 May 1;172(3):179-85.

Amitraz also diminished the inhibitory effects of the alpha (2)-adrenergic agonists clonidine and xylazine.
81(1,1,1,1) Details