CAS Number207679-81-0
Synonyms(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol; 2-[(1R)-3-(Diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol; (R)-5-Hydroxymethyl tolterodine; 5-hydroxymethyl tolterodine (PNU 200577); (R)-HYDROXYTOLTERODINE-D14; (R)-5-HYDROXYTOLTERODINE; R-(+)-2(3-DIISOPROPYLAMINO-1-PHENYLPROPYL)-4-HYDROXYMETHYLPHENOL; R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol; R-5-Hydroxymethyl Tolterodine; 3-[(1R)-3-[Bis(1-Methylethyl)Amino]-1-Phenylpropyl]-4-Hydroxy-Benzenemethanol; Desfesoterodine; 3-[(1R)-3-[BIS(1-METHYLETHYL)AMINO]-1-PHENYLPROPYL]-4-HYDROXYBENZENEMETHANOL; Fesoterodine fumarate Intermediate 2
Molecular FormulaC22H31NO2
Molecular Weight341.49
Purity98.00%
Density1.1±0.1 g/cm3
Boiling Point490.7±45.0 °C at 760 mmHg
Melting Point68-72°C
Appearancepowder
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 207679-81-0 |
| Catalog No. | 2A-9055409 |
| Chinese Name | (R)-5-羟甲基托特罗定 |
| Synonyms | (R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol; 2-[(1R)-3-(Diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol; (R)-5-Hydroxymethyl tolterodine; 5-hydroxymethyl tolterodine (PNU 200577); (R)-HYDROXYTOLTERODINE-D14; (R)-5-HYDROXYTOLTERODINE; R-(+)-2(3-DIISOPROPYLAMINO-1-PHENYLPROPYL)-4-HYDROXYMETHYLPHENOL; R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol; R-5-Hydroxymethyl Tolterodine; 3-[(1R)-3-[Bis(1-Methylethyl)Amino]-1-Phenylpropyl]-4-Hydroxy-Benzenemethanol; Desfesoterodine; 3-[(1R)-3-[BIS(1-METHYLETHYL)AMINO]-1-PHENYLPROPYL]-4-HYDROXYBENZENEMETHANOL; Fesoterodine fumarate Intermediate 2 |
| Molecular Formula | C22H31NO2 |
| Molecular Weight | 341.49 |
| Purity | 98.00 |
| Density | 1.1±0.1 g/cm3 |
| Boiling Point | 490.7±45.0 °C at 760 mmHg |
| Melting Point | 68-72°C |
| Appearance | powder |
| Storage Condition | -20?C Freezer |
| Application | (R)-5-Hydroxymethyl Tolterodine (PNU-200577; Desfesoterodine) is a muscarinic receptor antagonist with Kb and pA2 of 0.84 nM and 9.14, respectively. |
| HTC | 2922509090 |
| MDL Number | C22H31NO2 |
| SMILES | CC(C)N(CCC(c1ccccc1)c1cc(CO)ccc1O)C(C)C |
| InChI Key | DUXZAXCGJSBGDW-HXUWFJFHSA-N |
| MSDS | msds/55409_1_207679_81_0.pdf |
| Use of | (R)-5-Hydroxymethyl Tolterodine(PNU-200577; Desfesoterodine) is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively. IC50 value: 0.84 nM (Kb)Target: mAChR(R)-5-Hydroxymethyl Tolterodine is a major pharmacologically active metabolite of tolterodine. In vitro, (R)-5-Hydroxymethyl Tolterodine prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, (R)-5-Hydroxymethyl Tolterodine was significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, (R)-5-Hydroxymethyl Tolterodine was not selective for any muscarinic receptor subtype. Thus, (R)-5-Hydroxymethyl Tolterodine is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that (R)-5-Hydroxymethyl Tolterodine contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding. Properties Name 5-hydroxymethyl Tolterodine Synonym More Synonyms Biological Activity Description (R)-5-Hydroxymethyl Tolterodine(PNU-200577; Desfesoterodine) is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively. IC50 value: 0.84 nM (Kb)Target: mAChR(R)-5-Hydroxymethyl Tolterodine is a major pharmacologically active metabolite of tolterodine. In vitro, (R)-5-Hydroxymethyl Tolterodine prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, (R)-5-Hydroxymethyl Tolterodine was significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, (R)-5-Hydroxymethyl Tolterodine was not selective for any muscarinic receptor subtype. Thus, (R)-5-Hydroxymethyl Tolterodine is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that (R)-5-Hydroxymethyl Tolterodine contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding. Related Catalog Signaling Pathways >> GPCR/G Protein >> mAChR Signaling Pathways >> Neuronal Signaling >> mAChR Research Areas >> Neurological Disease References [1]. Nilvebrant L, Gillberg PG, Sparf B. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72. [2]. Fullhase, Claudius; Soler, Roberto; Gratzke, Christian et al. Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction. Journal of Urology (New York, NY, United States) (2010), 184(2), 783-789. [3]. Nilvebrant, Lisbeth Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacology & Toxicology (Oxford, United Kingdom) (2002), 90(5), 260-267. Chemical & Physical Properties Molecular Formula C22H31NO2 Exact Mass 341.235474 PSA 43.70000 Index of Refraction 1.563 InChIKey DUXZAXCGJSBGDW-HXUWFJFHSA-N Storage condition -20?C Freezer Safety Information HS Code 2922509090 Synthetic Route (R)-(4-(Benzylo... 156755-37-2 5-hydroxymethyl... 207679-81-0 3-[(1R)-3-Bisis... 1294517-15-9 5-hydroxymethyl... 207679-81-0 (R)-6-hydroxyme... 960373-33-5 Diisopropylamin... 5-hydroxymethyl... 207679-81-0 Precursor & DownStream Precursor 7 CAS#:156755-37-2 (R)-(4-(Benzylo... CAS#:1294517-15-9 3-[(1R)-3-Bisis... CAS#:108-18-9 Diisopropylamine CAS#:1333234-72-2 (R)-2-[3-(diiso... DownStream 3 CAS#:286930-02-7 Fesoterodine CAS#:1208313-13-6 O-Isobutyryl (R... CAS#:380636-50-0 3-[(1R)-3-(Diis... |
| Tax Rebate | 13.0% |
| Supervision | A. Customs clearance form for inbound goods B. Customs clearance form for outbound goods |
| Inspection | R. Hygiene supervision and inspection of imported food S. Hygiene supervision and inspection of exported food |
| Transport Info | Product name: Supervision conditions A. Customs clearance form for inbound goods B. Customs clearance form for outbound goods |
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