Terodiline hydrochloride

Terodiline hydrochloride用途

Terodiline hydrochloride 是一种 M1 选择性的毒蕈碱受体 (muscarinic receptor; mAChR) 拮抗剂。对兔输精管 (M1),心房 (M2),膀胱 (M3),回肠肌 (M3) 的 Kb 分别为 15,160,280,和 198 nM。Terodiline hydrochloride 还是钙通道 (Ca2+) 阻断剂。Terodiline hydrochloride可用于治疗尿频和急迫性尿失禁。

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Terodiline hydrochloride名称

[ CAS 号 ]:
7082-21-5

[ 英文名 ]:
Terodiline hydrochloride

[英文别名 ]:

TERODILINE HYDROCHLORIDE
Bicor
Terodiline chloride
TD-758
Terodiline HCl

Terodiline hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 神经疾病

[ 靶点 ]

mAChR[1] Ca2+ channel[1]

[体内研究]

Terodiline(80mg/kg；S.C.)在抑制膀胱内压和卡巴胆碱诱导的唾液分泌(ID50分别为24mg/kg和35mg/kg)和增大瞳孔直径(ED50为59mg/kg)方面具有等功能[1]。动物模型：Fmale或雄性Hartley豚鼠(200-600 g)[1]剂量：80 mg/kg给药：皮下注射。结果：ID50为24±6 mg/kg。更高的剂量是依特哈尔。

[参考文献]

[1]. Noronha-Blob L, et al. (+/-)-Terodiline: an M1-selective muscarinic receptor antagonist. In vivo effects at muscarinic receptors mediating urinary bladder contraction, mydriasis and salivary secretion. Eur J Pharmacol. 1991 Aug 29;201(2-3):135-42.

Terodiline hydrochloride物理化学性质

[ 沸点 ]:
390.9ºC at 760 mmHg

[ 分子式 ]:
C₂₀H₂₈ClN

[ 分子量 ]:
317.89600

[ 闪点 ]:
168.9ºC

[ 精确质量 ]:
317.19100

[ PSA ]:
12.03000

[ LogP ]:
6.17810

Terodiline hydrochlorideMSDS

详细MSDS(安全技术说明书)

Terodiline hydrochloride安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H319-H400

[ 警示性声明 ]:
P273-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn,N

[ 风险声明 (欧洲) ]:
22-36-50

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ RTECS号 ]:
UH9970000

Terodiline hydrochloride文献

Action potentials, contraction, and membrane currents in guinea pig ventricular preparations treated with the antispasmodic agent terodiline.

J. Pharmacol. Exp. Ther. 290(3) , 1417-26, (1999)

Terodiline was widely prescribed for urinary incontinence before reports of adverse cardiac effects that included bradycardia, QT lengthening, and ventricular tachyarrhythmia. The present study on gui...

Comparison of the effects of NS-21 and terodiline on the QTc interval in dogs.

Gen. Pharmacol. 30(1) , 137-42, (1998)

1. NS-21 [(+/-)-4-diethylamino-1,1-dimethylbut-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate monohydrochloride monohydrate], its active metabolite, RCC-36, and terodiline, are mixed anticholinergic...

CYP2D6 and CYP2C19 genotypes of patients with terodiline cardiotoxicity identified through the yellow card system.

Br. J. Clin. Pharmacol. 50(1) , 77-80, (2000)

Terodiline has concentration dependent QT prolonging effects and thus the potential for cardiotoxicity. Pharmacogenetic variation in terodiline metabolism could be responsible for cardiotoxicity. We s...

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