| CAS NO: | 207679-81-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 341.49 |
|---|---|
| Formula | C22H31NO2 |
| CAS No. | 207679-81-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 68 mg/mL (199.1 mM) |
| Water: <1 mg/mL | |
| Ethanol: 68 mg/mL (199.1 mM) | |
| Other info | Chemical Name: (R)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol InChi Key: DUXZAXCGJSBGDW-HXUWFJFHSA-N InChi Code: InChI=1S/C22H31NO2/c1-16(2)23(17(3)4)13-12-20(19-8-6-5-7-9-19)21-14-18(15-24)10-11-22(21)25/h5-11,14,16-17,20,24-25H,12-13,15H2,1-4H3/t20-/m1/s1 SMILES Code: OC1=CC=C(CO)C=C1[C@@H](C2=CC=CC=C2)CCN(C(C)C)C(C)C |
| Synonyms | Desfesoterodine, PNU-200577; 5-HMT, 5-HM; PNU200577; PNU 200577 |
| In Vitro | In vitro activity: 5-hydroxymethyl tolterodine is a major pharmacologically active metabolite of tolterodine. 5-hydroxymethyl tolterodine produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips. 5-hydroxymethyl tolterodine antagotizes muscarinic receptors with a pA2 of 9.1. 5-hydroxymethyl tolterodine causes a concentration-dependent inhibition of (-)3 H-QNB binding in homogenates of guinea-pig urinary bladder, parotid gland, heart and cerebral cortex. 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. |
|---|---|
| In Vivo | 5-hydroxymethyl tolterodine is significantly more potent at inhibiting acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50 15 and 40 nmol/kg, respectively. 5-hydroxymethyl tolterodine is three times more potent at the urinary bladder compared to the salivary gland. |
| Animal model | Male guinea-pigs |
| Formulation & Dosage | Dissolved in saline; 2 nmol/kg -203 nmol/kg; i.v. injection |
| References | Pharmacol Toxicol. 1997 Oct;81(4):169-72. |
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