The Utility of the Artificial Taste Sensor in Evaluating the Bitterness of Drugs: Correlation with Responses of Human TASTE2 Receptors (hTAS2Rs)
The Utility of the Artificial Taste Sensor in Evaluating the Bitterness of Drugs: Correlation with Responses of Human TASTE2 Receptors (hTAS2Rs)
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DOI：
10.1248/cpb.c17-00619
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发表时间：
2018-01-01
影响因子：
1.7
通讯作者：
Ikezaki, Hidekazu
中科院分区：
文献类型：
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作者：
Haraguchi, Tamami;Uchida, Takahiro;Ikezaki, Hidekazu
本研究的目的是通过比较人工味觉传感器的响应与人类TASTE 2受体（hTAS 2 Rs）的记录响应来检查人工味觉传感器评估药物苦味的能力。为此目的，选择了22种苦味化合物进行测试，这些化合物在日本用作药物的成分，并且是已知的hTAS 2 Rs配体。通过五种不同的味觉传感器（ACO、ANO、BTO、COO、AE 1）评价它们的溶液（0.01、0.03、0.1mm）。评价了化合物的理化参数与味觉传感器和hTAS 2 Rs的响应之间的相关性。根据味觉传感器测量，预测地芬尼多、氟哌啶醇、苯海拉明、美沙芬和罂粟碱（hTAS 2 R10和/或hTAS 2 R14的所有配体）表达强苦味，超过奎宁的苦味。发现味觉传感器BTO的响应与hTAS 2 R14的响应显著相关。高logP值（>= 2.73）和hTAS 2 R14的应答也显著相关（**p
The purpose of this study was to examine the ability of the artificial taste sensor to evaluate the bitterness of drugs by comparing the responses of the taste sensor with documented responses of human TASTE2 receptors (hTAS2Rs). For this purpose 22 bitter compounds, used as ingredients of pharmaceutical medicines in Japan and known ligands of hTAS2Rs, were selected for testing. Their solutions (0.01, 0.03, 0.1 mm) were evaluated by five different taste sensors (ACO, ANO, BTO, COO, AE1). Correlations between physicochemical parameters of the compounds and the responses of the taste sensors and hTAS2Rs were evaluated. From taste sensor measurements, diphenidol, haloperidol, diphenhydramine, dextromethorphan and papaverine, all ligands of hTAS2R 10 and/or hTAS2R14, were predicted to express strong bitterness, surpassing that of quinine. Responses of taste sensors BTO were found to be significantly correlated with responses of hTAS2R14. High logP values (>= 2.73) and responses of hTAS2R14 were also significantly correlated (**p