1. GPCR/G Protein Neuronal Signaling Others
  2. mAChR Isotope-Labeled Compounds
  3. (R)-Hydroxytolterodine-d14

(R)-Hydroxytolterodine-d14  (Synonyms: PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14)

Cat. No.: HY-76569S1
Handling Instructions

(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.

For research use only. We do not sell to patients.

(R)-Hydroxytolterodine-d<sub>14</sub> Chemical Structure

(R)-Hydroxytolterodine-d14 Chemical Structure

CAS No. : 1191280-58-6

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Description

(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively[1]. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053)[2][3]. Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats[4].

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
In vitro, Desfesoterodine preventes carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner[2].
In radioligand binding studies carries out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, Desfesoterodine is not selective for any muscarinic receptor subtype[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Desfesoterodine (PNU-200577; 5-Hydroxymethyl Tolterodine; 0.1 and 1 mg/kg; IV) significantly increases bladder compliance after moderate and high doses[5].
In vivo, Desfesoterodine is 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) [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

355.57

Formula

C22H17D14NO2

CAS No.
Unlabeled CAS

207679-81-0

SMILES

OC1=CC=C(CO)C=C1[C@H](CCN(C([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])C([2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])C2=CC=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
(R)-Hydroxytolterodine-d14
Cat. No.:
HY-76569S1
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