5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)
For research use only.
Catalog No.S2659 Synonyms: Desfesoterodine
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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|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.|
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. |
|In vitro||DMSO||68 mg/mL (199.12 mM)|
|Ethanol||68 mg/mL (199.12 mM)|
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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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