Detrol LA
Tolterodine Tartrate
CAS: 124937-52-6
Molecular Formula: C26H37NO7
Detrol LA - Names and Identifiers
| Name | Tolterodine Tartrate |
| Synonyms | Detrol Detrol LA Detrusitol PNU 200583E PNU-200583E UNII-5T619TQR3R Tolterodine Tartrate Tolterodine L-Tartrate Tolterodine-L-tartrate Tolterodine Tartrate API Tolterodine Tartaric Acid Tolterodine tartrate [USAN] (±)-Tolterodine-d14 Tartrate R-(+)-Toltaridine L-Tartrate Tolterodine tartrate (Detrol LA) R-(+)-N,N-Diisopropyl-3-(2-hydroxy-5-Methylphenyl)-3-phenylpropylaMine L-Tartarte 2-{(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl}-4-methylphenol 2,3-dihydroxybutanedioate (salt) |
| CAS | 124937-52-6 |
| EINECS | 620-503-4 |
| InChI | InChI=1/C22H31NO.C4H6O6/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24;5-1(3(7)8)2(6)4(9)10/h6-12,15-17,20,24H,13-14H2,1-5H3;1-2,5-6H,(H,7,8)(H,9,10)/t20-;/m1./s1 |
Detrol LA - Physico-chemical Properties
| Molecular Formula | C26H37NO7 |
| Molar Mass | 475.57 |
| Melting Point | 205-210°C |
| Boling Point | 442.2°C at 760 mmHg |
| Specific Rotation(α) | 54625 +36.0° |
| Flash Point | 192.1°C |
| Solubility | Soluble in water (0.012 mg/ml), DMSO (≥20 mg/ml), methanol, and ethanol (6 mg/ml) |
| Vapor Presure | 1.97E-08mmHg at 25°C |
| Appearance | White to white-like powder |
| Color | White to Off-White |
| pKa | 9.87(at 25℃) |
| Storage Condition | Sealed in dry,2-8°C |
| MDL | MFCD07771985 |
| Physical and Chemical Properties | Melting point 205-210°C |
| Use | Used as an anti-incontinence treatment |
| In vitro study | Tolterodine has high affinity and specificity for muscarinic receptors in vitro and it exhibits bladder and salivary gland selectivity in vivo. Tolterodine is a new muscarinic receptor antagonist used in the treatment of urge incontinence and related overactive bladder symptoms. Tolterodine effectively inhibited carbachol-induced contractions in guinea pig bladder isolation strips in a concentration-dependent, competitive manner. Tolterodine muscarinic receptors have high affinity binding in guinea pig bladder (Ki 2.7 nM), heart (Ki 1.6 nM), cerebral cortex (Ki 0.75 nM), parotid gland (Ki 4.8 nM), in the human bladder (Ki 3.3 nM). |
| In vivo study | In anesthetized cats, Tolterodine(1 mg/kg, I. P.) significantly inhibited acetylcholine-induced bladder contractions more effectively than electrosalivation. Intravenous administration of Tolterodine increased the mean voiding interval, bladder capacity, and voiding volume in normal rats and in arabesin-treated rats. In control cerebral infarcted rats, Tolterodine(2 nM/kg) significantly increased bladder capacity (BC) without increasing residual capacity, but it had no effect on resiniferatoxin-BC in cerebral infarcted rats. In female rats with bladder outlet obstruction, Tolterodine tartrate (0.1 and 1.0 mg/kg) significantly reduced the number and amplitude of nonvoiding contractions by 38-74% and 29-44%, respectively, and increase bladder capacity by 19-51%. |
Detrol LA - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S37/39 - Wear suitable gloves and eye/face protection |
| UN IDs | UN 2811 6.1 / PGIII |
| HS Code | 29222990 |
| Toxicity | LD50 i.v. in male mice: 10-20 mg/kg (Jnsson) |
Detrol LA - Nature
Open Data Verified Data
white crystalline powder; Odorless, bitter. Dissolved in methanol, slightly soluble in water, slightly soluble in acetic acid, very slightly soluble in acetone, chloroform and ether almost insoluble.
Last Update：2025-06-10 22:55:16
Detrol LA - Application
Open Data Verified Data
developed by Pharmacia & Upiohn, Inc., USA, which was first launched in Sweden in February 1998 and in the United Kingdom and the United States in the same year. It was launched in France in April 1999. Muscarinic receptor antagonists. For the treatment of bladder stimulation caused by urinary incontinence, urinary frequency and urgency and other symptoms.
Last Update：2025-08-19 16:24:40
Detrol LA - Introduction
Tolterodine tartrate is a Tolterodine tartrate form and is a competitive muscarinic acetylcholine receptor antagonist.
Last Update：2022-10-16 17:12:57
Detrol LA - Safety
Open Data Verified Data
male mice were injected intravenously with LDso: 10~20mg/kg.
Last Update：2022-01-01 09:24:26
Detrol LA - Reference Information
| Introduction | Tolteridine tartrate is a competitive M receptor antagonist, and its selectivity for the bladder is significantly stronger than that for the salivary glands. The inhibition of bladder contraction is about 20 times that of the salivary glands. It is mainly used as a therapeutic drug for anti-urinary incontinence, and can also treat polyuria in the elderly. |
| Biological activity | Tolterodine tartrate (PNU-200583E) is a Tolterodine tartrate form and a competitive muscarinic acetylcholine receptor antagonist. |
| Target | Value |
| Use | Used as a therapeutic drug for anti-urinary incontinence Treating polyuria in the elderly. |
Last Update：2024-04-09 19:55:45
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CAS: 124937-52-6
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