Denatonium benzoate -d 5 (THS-839-d 5 ) is the deuterium labeled Denatonium benzoate. Denatonium benzoate (THS-839) is known as the most bitter compound and is commonly used as a deterrent (bittering agent) to activate different types of bitter taste receptors (TAS2Rs) with oral activity. Denatonium benzoate can enhance insulin secretion, has anti-inflammatory effects, and promotes allergy susceptibility [1] [2] [3] [4].
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Plamen I Zagorchev, et al. Denatonium benzoate decreases the effect of histamine in vitro and in rats. Tropical Journal of Pharmaceutical Research September.2020; 19 (9): 1879-1885.
[2]. Huaping Xu, et al. Denatonium Benzoate Exposure Promotes IgE-Mediated Mast Cell Degranulation and Allergy By Upregulating FcεRIα Expression.Hypothesis. posted 29 Sep, 2021
[3]. DALEE. KAUKEINEN, et al. Evaluation of aversive agents to increase the selectivity of rodenticides with emphasis on denatonium benzoate (Bitrex) bittering agent. eScholarship. Proceedings of the Vertebrate Pest Conference, 15(15)
[4]. Weikun Huang, et al. Effects of a bitter substance, denatonium benzoate, on pancreatic hormone secretion. Am J Physiol Endocrinol Metab. 2024 Apr 1;326(4):E537-E544.
In Vitro, Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
References:
[1]. Plamen I Zagorchev, et al. Denatonium benzoate decreases the effect of histamine in vitro and in rats. Tropical Journal of Pharmaceutical Research September.2020; 19 (9): 1879-1885.
[2]. Huaping Xu, et al. Denatonium Benzoate Exposure Promotes IgE-Mediated Mast Cell Degranulation and Allergy By Upregulating FcεRIα Expression.Hypothesis. posted 29 Sep, 2021
[3]. DALEE. KAUKEINEN, et al. Evaluation of aversive agents to increase the selectivity of rodenticides with emphasis on denatonium benzoate (Bitrex) bittering agent. eScholarship. Proceedings of the Vertebrate Pest Conference, 15(15)
[4]. Weikun Huang, et al. Effects of a bitter substance, denatonium benzoate, on pancreatic hormone secretion. Am J Physiol Endocrinol Metab. 2024 Apr 1;326(4):E537-E544.