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124937-51-5

124937-51-5 structure
124937-51-5 structure
  • Name: Tolterodine-L-tartrate
  • Chemical Name: tolterodine
  • CAS Number: 124937-51-5
  • Molecular Formula: C22H31NO
  • Molecular Weight: 325.488
  • Catalog: API Urinary system medication Diuretic
  • Create Date: 2018-09-20 18:38:43
  • Modify Date: 2024-01-02 14:02:29
  • Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. IC50 Value:Target: mAChRin vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors [1].in vivo: Tolterodine was extensively metabolized in vivo [2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased [3].

Name tolterodine
Synonyms MFCD07771985
(+)-Tolterodine
2-[(1R)-3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol
(R)-2-[3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-methylphenol
(R)-Tolterodine
tolterodine
Detrol
Tolterodine L-tartrate
Detrusitol
Phenol, 2-((1R)-3-(bis(1-methylethyl)amino)-1-phenylpropyl)-4-methyl-
TOLTERODINE TARTRATE
(+)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine
(+)-(R)-2-[a-[2-(Diisopropylamino)ethyl]benzyl]-p-cresol
Phenol, 2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-methyl-
Description Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. IC50 Value:Target: mAChRin vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors [1].in vivo: Tolterodine was extensively metabolized in vivo [2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased [3].
Related Catalog
References

[1]. Nilvebrant L. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7.

[2]. Andersson SH, et al. Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs. Drug Metab Dispos. 1998 Jun;26(6):528-35.

[3]. Cappon GD, et al. Tolterodine does not affect memory assessed by passive-avoidance response test in mice. Eur J Pharmacol. 2008 Jan 28;579(1-3):225-8.

Density 1.0±0.1 g/cm3
Boiling Point 442.2±45.0 °C at 760 mmHg
Molecular Formula C22H31NO
Molecular Weight 325.488
Flash Point 192.1±27.4 °C
Exact Mass 325.240570
PSA 23.47000
LogP 5.77
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.548
Storage condition -20°C Freezer
Hazard Codes Xn,Xi
Risk Phrases R22:Harmful if swallowed.
Safety Phrases S36/37/39
RIDADR 1987
WGK Germany 2