90043-86-0
Chemical Structure
Ipidacrine hydrochloride
Synonym(s): NIK-247; Amiridine
- CAS No.: 90043-86-0
- Formula:C12H17ClN2
- Molecular Weight:224.73
IUPAC Name: 2,3,5,6,7,8-hexahydro-1H-cyclopenta[b]quinolin-9-amine hydrochloride
InChIKey: FERZJAONQGPFCU-UHFFFAOYSA-N
SMILES: NC1=C2C(CCCC2)=NC3=C1CCC3.Cl
Biological Activity: Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-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 hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride 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].
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Ipidacrine hydrochloride | Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-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 hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride 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. | |||||||||||||||||||||
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References
- [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.
