5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

For research use only.

Catalog No.S2659 Synonyms: Desfesoterodine

5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM) Chemical Structure

CAS No. 207679-81-0

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

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Biological Activity

Description 5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.
Features A competitive antagonist at the muscarinic receptors.
Targets
mAChR [1]
0.84 nM(Kb)
In vitro

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. [1] 5-hydroxymethyl tolterodine has a similar pharmacological profile with tolterodine. [2] Intravenous infusion of 5-hydroxymethyl tolterodine produces a dose-dependent inhibition of the intravesical volume-induced urinary bladder contraction measured as the micturition pressure. [3]

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. [1]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: Male guinea-pigs
  • Dosages: 2 nmol/kg -203 nmol/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (199.12 mM)
Ethanol 68 mg/mL (199.12 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 341.49
Formula

C22H31NO2

CAS No. 207679-81-0
Storage powder
in solvent
Synonyms Desfesoterodine
Smiles CC(C)N(CCC(C1=CC=CC=C1)C2=C(C=CC(=C2)CO)O)C(C)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01964183 Completed Drug: tolterodine|Drug: mirabegron Pharmacokinetics of Mirabegron and Tolterodine|Healthy Astellas Pharma Inc June 2013 Phase 4
NCT01521767 Completed Drug: tolterodine tartrate Urinary Bladder Overactive Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer October 2011 Phase 1
NCT01286454 Completed Drug: fesoterodine Overactive Bladder (OAB) With Symptoms of Frequency Urgency and Urgency Pfizer December 2010 Phase 1
NCT00902681 Completed Drug: Fesoterodine Treatment of Overactive Bladder Pfizer June 2009 Phase 1
NCT00911235 Completed Drug: Fesoterodine|Drug: fesoterodine plus fluconazole Overactive Bladder With Symptoms of Frequency Urgency and Urge Urinary Incontinence Pfizer May 2009 Phase 1

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AChR Signaling Pathway Map

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