Terodiline hydrochloride
(Synonyms: 盐酸特罗地林) 目录号 : GC39186
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。
Cas No.:7082-21-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence[1].
[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.
| Cas No. | 7082-21-5 | SDF | |
| 别名 | 盐酸特罗地林 | ||
| Canonical SMILES | CC(NC(C)(C)C)CC(C1=CC=CC=C1)C2=CC=CC=C2.[H]Cl | ||
| 分子式 | C20H28ClN | 分子量 | 317.9 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1456 mL | 15.7282 mL | 31.4564 mL |
| 5 mM | 0.6291 mL | 3.1456 mL | 6.2913 mL |
| 10 mM | 0.3146 mL | 1.5728 mL | 3.1456 mL |
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动物平均体重 | g | |
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Stereoselective cardiotoxic effects of terodiline
Clin Pharmacol Ther 1996 Jul;60(1):89-98.PMID:8689817DOI:10.1016/S0009-9236(96)90171-X.
Objective: To study the cardiovascular and electrocardiographic (ECG) effects of the R(+)- and S(-)- enantiomers of terodiline. The racemic drug was previously used to treat detrusor instability but was withdrawn after it caused serious ventricular arrhythmias associated with prolongation of the QT interval. Methods: A double-blind, placebo-controlled, randomized crossover study was performed that involved nine healthy volunteers who were given single oral doses of racemic Terodiline hydrochloride (200 mg), R(+)-terodiline hydrochloride (100 mg), S(-)-terodiline tartrate (100 mg), or placebo. Plasma concentrations of each enantiomer and cardiovascular and ECG effects, including QT intervals and QT dispersion, were measured over 14 days after each treatment. Results: Both racemic and R(+)-terodiline significantly increased QT interval, corrected QT interval (QTc), and QRS duration (all p < 0.05), without affecting QT dispersion. S(-)-Terodiline tartrate (100 mg) did not affect QTc. Peak effects occurred 8 hours after dosing when increases in QTc from baseline (95% confidence intervals) were -3 (-20, 13) for placebo, 23 (8, 37) for racemic terodiline, 19 (6, 33) for R(+)-terodiline, and 0 (-10, 9) ms1/2 for S(-)-terodiline. Although differences were observed between the pharmacokinetics of the two enantiomers, these were not sufficient to account for the differences in ECG effects, and elimination half-lives were similar. Elimination of terodiline enantiomers was not significantly delayed in two genotypic poor metabolizers of debrisoquin (CYP2D6). Conclusions: QT prolongation associated with racemic terodiline is caused exclusively by the R(+)-enantiomer, which therefore appears to be responsible for the ventricular arrhythmias caused by the drug.
[Clinical effects of Terodiline hydrochloride on urinary frequency and sense of residual urine--a double blind clinical trial using flavoxate hydrochloride as a control]
Hinyokika Kiyo 1988 Apr;34(4):739-53.PMID:3041785doi
A double blind clinical trial was performed as a multicenter study to determine the usefulness of Terodiline hydrochloride (HCl), an anticholinergic and calcium antagonistic agent, for urinary frequency or sense of residual urine in patients with psychogenic diseases, chronic prostatitis or chronic cystitis. Either 24 mg of terodiline HCl a day or 600 mg of flavoxate HCl a day was given for 4 weeks. One hundred and ninety-nine patients completed the test. The final global improvement rating was 70% in patients given terodiline HCl and 48% in patients given flavoxate HCl. The difference was statistically significant (p less than 0.01). Diurnal and nocturnal urinary frequency and urinary incontinence were less in patients given terodiline HCl than in patients given flavoxate HCl (p less than 0.01). No difference was noted between the two agents in relieving sense of residual urine. Compared with the control period, the average urinary frequency decreased 2.0 times a day in patients given terodiline HCl and 0.7 times in patients given flavoxate HCl. The difference was statistically significant (p less than 0.01). Adverse effects were observed in 12% of the patients given terodiline HCl and in 16% of the patients given flavoxate HCl. They included thirst, difficult urination, constipation, slight increase of serum GOT, GPT or alkaline phosphatase, and so forth. They disappeared with discontinued use of the agent. The global utility rating was 68% in patients given terodiline HCl and 45% in patients given flavoxate HCl, the difference being significant (p less than 0.01). These results indicate that terodiline HCl is useful for the treatment of urinary symptoms in patients with psychogenic diseases, chronic prostatitis or chronic cystitis.
[Clinical studies of Terodiline hydrochloride and clenbuterol hydrochloride for urinary frequency and incontinence]
Hinyokika Kiyo 1991 Nov;37(11):1575-80.PMID:1767784doi
The clinical effectiveness and safety of Terodiline hydrochloride and clenbuterol hydrochloride were studied on 51 patients with neurogenic bladder, stress incontinence, unstable bladder and others, the chief complaints of which were urinary frequency or urinary incontinence. Overall improvement was graded as marked in 6 patients (11.8%), moderate in 20 patients (39.2%), slight in 11 patients (21.6%), unchanged in 13 patients (25.5%) and aggravated in one. The patients impression was "good" or better in 56.9%. There were a total of 13 cases (25.5%) of adverse reactions, namely, 7 cases of finger tremor, 3 cases of dry mouth and others. These reactions disappeared rapidly after the discontinuance of drug administration. The clinical efficacy in the treatment of subjective symptoms was 71.4% for urinary incontinence, 56.4% for diurnal pollakisuria. The examination of lower urethral functions demonstrated a significant (p less than 0.01) increase in bladder capacity at first desire and maximum desire to void. However, we found no significant increase in urethral clossure pressure. The findings of this study suggest that Terodiline hydrochloride and clenbuterol hydrochloride are very useful for the treatment of urinary frequency and incontinence.
In vivo and in vitro electrophysiologic effects of terodiline on dog myocardium
J Cardiovasc Electrophysiol 1995 Jun;6(6):443-54.PMID:7551314DOI:10.1111/j.1540-8167.1995.tb00418.x.
Introduction: Terodiline hydrochloride, widely prescribed for urinary incontinence, has been reported to cause bradycardia and torsades de pointes. Methods and results: In this study, we characterized the electrophysiologic effects of terodiline in dog cardiac tissues in vivo and in isolated canine cardiac Purkinje fibers. Terodiline (1 to 10 microM) resulted in dose-dependent reduction of action potential amplitude and maximal upstroke velocity (Vmax). The threshold for these effects was approximately 2 microM (0.6 mg/L), and the changes were cycle-length dependent. Terodiline (> or = 2 microM) also depressed the action potential plateau but did not significantly alter action potential duration at concentrations < or = 10 microM. In vivo studies demonstrated that high doses of terodiline (3 mg/kg) lengthened AH and HV intervals, slowed spontaneous sinus rate, prolonged ventricular refractoriness, and inhibited vagally induced slowing of the sinus node. Sympathetic effects on spontaneous sinus rate were unchanged. In both isolated canine Purkinje fibers and anesthetized dogs, terodiline did not evoke afterdepolarizations, repetitive firing, or ventricular tachyarrhythmias under normal or hypokalemic conditions. Conclusion: Our findings suggest that terodiline (> or = 1 to 2 microM) leads to blockade of sodium and calcium channels as well as muscarinic receptors in canine cardiac tissues.
A review of flavoxate hydrochloride in the treatment of urge incontinence
J Int Med Res 1988 Sep-Oct;16(5):317-30.PMID:2461883DOI:10.1177/030006058801600501.
This article provides a review of the use of flavoxate hydrochloride in the treatment of urge incontinence. It outlines the pharmacology, mode of action, toxicology and pharmacokinetic studies which have been carried out, and then reviews the clinical studies, including those involving patients with benign prostatic hypertrophy. The effects of dosages of 600-1200 mg/day are compared, particularly regarding safety and tolerability factors. Finally, alternative therapies to flavoxate hydrochloride (alpha-adrenergic receptor blockers, oxybutinin chloride, Terodiline hydrochloride, emepronium bromide and imipramine) are summarized. The article is written in the knowledge of recent evidence which indicates that flavoxate hydrochloride exhibits only weak anticholinergic activity on receptors involved in the control of the lower urinary tract.