Ipidacrine-d₁₀  (Synonyms: NIK-247-d₁₀ free base)

Ipidacrine-d₉ (NIK-247-d₉ (free base)) is the deuterium labeled Ipidacrine (HY-W027553). Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC₅₀ values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases^{[1][2][3][4][5]}.

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].

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

198.33

C₁₂H₆D₁₀N₂

62732-44-9

[2H]C1(C2=C(C([2H])(C([2H])(C1([2H])[2H])[2H])[2H])N=C3C([2H])(CCC3=C2N)[2H])[2H]

Room temperature in continental US; may vary elsewhere.

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

• [1]. Kojima J, et al. Ipidacrine (NIK-247): A Review of Multiple Mechanisms as an Antidementia Agent[J]. CNS Drug Reviews, 1998, 4(3): 247-259.

  [2]. Pulatov S S. Efficacy of ipidacrine in the recovery period of ischaemic stroke[J]. World Bulletin of Public Health, 2022, 7: 28-32.

  [3]. Bykov V, et al. Ipidacrine (Axamon), A Reversible Cholinesterase Inhibitor, Improves Erectile Function in Male Rats With Diabetes Mellitus-Induced Erectile Dysfunction[J]. Sex Med. 2022 Feb;10(1):100477.  [Content Brief]

  [4]. Zinovyeva O E, et al. Ipidacrine efficacy in diabetic polyneuropathy complex treatment: A review[J]. Consilium Medicum, 2022, 24(2): 123-127.

  [5]. Samartsev I N, et al. The efficacy and safety of ipidacrine in patients with idiopathic neuropathy of the facial nerve (PELICAN study)[J]. Neurology, Neuropsychiatry, Psychosomatics, 2022, 14(1): 60-68.