CAS 124937-51-5|Tolterodine-L-tartrate

Introduction：Basic information about CAS 124937-51-5|Tolterodine-L-tartrate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Tolterodine-L-tartrate BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	Tolterodine-L-tartrate
CAS Number	124937-51-5	Molecular Weight	325.488
Density	1.0±0.1 g/cm3	Boiling Point	442.2±45.0 °C at 760 mmHg
Molecular Formula	C₂₂H₃₁NO	Melting Point	/
MSDS	/	Flash Point	192.1±27.4 °C

Names

Name	tolterodine
Synonym	More Synonyms

Tolterodine-L-tartrate BiologicalActivity

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	Signaling Pathways >>GPCR/G Protein >>mAChRSignaling Pathways >>Neuronal Signaling >>mAChRResearch Areas >>Neurological Disease
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.

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

Signaling Pathways >>GPCR/G Protein >>mAChRSignaling Pathways >>Neuronal Signaling >>mAChRResearch Areas >>Neurological Disease

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.

Chemical & Physical Properties

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
InChIKey	OOGJQPCLVADCPB-HXUWFJFHSA-N
SMILES	Cc1ccc(O)c(C(CCN(C(C)C)C(C)C)c2ccccc2)c1
Storage condition	-20°C Freezer

Safety Information

Hazard Codes	Xn,Xi
Risk Phrases	R22:Harmful if swallowed.
Safety Phrases	S36/37/39
RIDADR	1987
WGK Germany	2

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-

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