5-Hydroxymethyl Tolterodine-d14 (formate)

5-Hydroxymethyl Tolterodine-d14 (formate)

• UNSPSC Description: 5-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
• Target Antigen: Isotope-Labeled Compounds; mAChR
• Type: Isotope-Labeled Compounds
• Related Pathways: GPCR/G Protein;Neuronal Signaling;Others
• Applications: Neuroscience-Neuromodulation
• Field of Research: Neurological Disease
• Solubility: 10 mM in DMSO
• Smiles: [2H]C([2H])([2H])C(C([2H])([2H])[2H])([2H])N(C(C([2H])([2H])[2H])([2H])C([2H])([2H])[2H])CC[C@H](C1=CC=CC=C1)C2=CC(CO)=CC=C2O.OC([H])=O
• Molecular Weight: 401.60
• References & Citations: [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.|[2]B Malhotra, et al. The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9.|[3]L Nilvebrant, et al. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72.|[4]Shizuo Yamada, et al. Muscarinic receptor binding of fesoterodine, 5-hydroxymethyl tolterodine, and tolterodine in rat tissues after the oral, intravenous, or intravesical administration. J Pharmacol Sci. 2019 May;140(1):73-78.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported