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Ipidacrine Sale

(Synonyms: 伊匹达克林) 目录号 : GC49299

An AChE inhibitor

Ipidacrine Chemical Structure

Cas No.:62732-44-9

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产品描述

Ipidacrine is an inhibitor of acetylcholinesterase (AChE; IC50 = 270 nM).1 It induces long-term potentiation (LTP) in rat hippocampal slices, an effect that can be blocked by the muscarinic antagonists atropine or pirenzepine , when used at a concentration of 10 µM.2 Ipidacrine (0.03-1 mg/kg) prevents memory deficits induced by the anticholinergic agent scopolamine in the passive avoidance test in rats.2

1.Ogura, H., Kosasa, T., Kuriya, Y., et al.Comparison of inhibitory activities of donepezil and other cholinesterase inhibitors on acetylcholinesterase and butyrylcholinesterase in vitroMethods Find. Exp. Clin. Pharmacol.22(8)609-613(2000) 2.Yoshida, S., and Suzuki, N.Antiamnesic and cholinomimetic side-effects of the cholinesterase inhibitors, physostigmine, tacrine and NIK-247 in ratsEur. J. Pharmacol.250(1)117-124(1993)

Chemical Properties

Cas No. 62732-44-9 SDF
别名 伊匹达克林
Canonical SMILES NC1=C(CCC2)C2=NC3=C1CCCC3
分子式 C12H16N2 分子量 188.3
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Research Update

Ipidacrine (Axamon), A Reversible Cholinesterase Inhibitor, Improves Erectile Function in Male Rats With Diabetes Mellitus-Induced Erectile Dysfunction

Sex Med 2022 Feb;10(1):100477.PMID:35007992DOI:10.1016/j.esxm.2021.100477.

Background: Management of diabetes mellitus-induced erectile dysfunction (DMED) is challenging because of its insufficient responses to phosphodiesterase type 5 inhibitors. Aim: To compare the effects of Ipidacrine, a reversible cholinesterase inhibitor, and sildenafil on DMED in a rat model of streptozotocin (STZ)-induced diabetes. Methods: Erectile dysfunction (ED) caused by STZ-induced diabetes mellitus was modeled in adult male Wistar rats, which were randomized to 4 groups: untreated diabetic rats, sildenafil (5 mg/kg), Ipidacrine (3.6 mg/kg) and Ipidacrine (6.7 mg/kg). The test drug (Ipidacrine), comparator (sildenafil) or control substance (1% starch solution) were administered orally for 5 days or 14 days. Erectile function was assessed by the change in the maximum intracavernous pressure (ICPmax) following cavernous nerve electrical stimulation. The mean arterial pressure (MAP) was recorded, and the ICPmax/MAP ratio was calculated. Sexual behavior, cholinesterase activity and blood testosterone level tests assessed. Main outcome measure: The quantitative value of ICPmax/MAP 14 days after the start of administration of the test drug and the comparison drug. Results: Animals with STZ-induced diabetes mellitus showed a significant decrease in ICPmax and ICPmax/MAP ratio compared to the intact control group. When Ipidacrine was administered to rats with DMED for 14 days, an increase in these indicators was noted. It was proved that Ipidacrine at a dose of 6.7 mg/kg has noninferiority compared to sildenafil on the DMED model. Significant increase in ICPmax compared to STZ-control after electrostimulation of the cavernous nerve was recorded following administration of Ipidacrine at a dose of 6.7 mg/kg (P < .05) and sildenafil at a dose 5 mg/kg (P < .05). Neither the test drug, nor the comparator were associated with increase in testosterone levels in blood; as well both drugs did not promote activation of sexual behavior. Clinical implications: Ipidacrine may be considered as an effective therapy for DMED but needs to be verified in human investigations. Strengths & limitations: The role of Ipidacrine, was firstly demonstrated in rats with DMED. However, the results were obtained in animal experiments, and will be further tested in the study of receptor interactions and the determination of cellular targets. Conclusion: This is the first study to show that administration of Ipidacrine, the reversible cholinesterase inhibitor, improved erectile function in diabetic rats and these results may be beneficial in further studies using Ipidacrine for treatment of DMED, particularly in non-responders to PDE5 inhibitors. Bykov V, Gushchina E, Morozov S, et al. Ipidacrine (Axamon), A Reversible Cholinesterase Inhibitor, Improves Erectile Function in Male Rats With Diabetes Mellitus-Induced Erectile Dysfunction. Sex Med 2022;10:100477.

[Compression of nerves and senses: Ipidacrine as the light at the end of the tunnel]

Zh Nevrol Psikhiatr Im S S Korsakova 2021;121(2):31-37.PMID:33728848DOI:10.17116/jnevro202112102131.

Objective: To evaluate the efficacy of the AChE inhibitor Ipidacrine when added to traditional therapy in outpatients with tunnel syndromes (TS) based on clinical, neurophysiological and psycho-emotional indicators. Material and methods: Ninety-two patients with a verified diagnosis of TS were randomized into a main group (MG), in which Ipidacrine was added to the therapy (n=50), and a control group (CG), which received conventional therapy (n=42). Clinical neurological examination, provocative (Tinel, Falen, Goldberg finger compression, elevator and tourniquet) tests, pain questionnaires (VAS, DN4, PainDetect, Pain Disability Index), Beck's depression scale, the Spielberger Trait and State Anxiety Inventory, electroneuromyography (ENMG) were used. Results: Most of the examined subjects were patients with mild TS without muscle weakness or amyotrophy (80%). In the main group, there was a significant decrease in hypoesthesia, normalization of provocative tests, the increase of SNAP amplitudes, as well as nerve conduction velocities over motor and sensory fibers of the studied nerves (p<0.05). Besides, the regression of neuropathic pain syndrome was objectified according to VAS, DN4 and PainDetect scales, which indexes decreased significantly (p<0.01) in the course of therapy combined with Ipidacrine. The positive dynamics, in its turn, contributed to the reduction of depression according to Beck's depression scale, comorbid chronic pain syndrome and improvement of patients' quality of life according to Pain Disability Index (p<0.05). There was no significant improvement of clinical and neurophysiological parameters in the CG (p>0.05). There were no significant differences in the assessment of pain, depression and quality of life (p>0.05), except for a decrease in VAS scores (p=0.03). Conclusion: In patients treated with traditional therapy in combination with Ipidacrine, the follow-up study after 4 weeks showed the reliable positive dynamics of clinical, neurophysiological and psycho-emotional indicators without application of psychoactive drugs.

Ipidacrine in combination therapy regimens of functional constipation

Ter Arkh 2018 Dec 30;90(12):48-55.PMID:30701833DOI:10.26442/00403660.2018.12.000008.

Aim: Analysis of the treatment response rates of different therapy regimens of functional constipation, including Ipidacrine, a cholinesterase inhibitor, based on assessment of adaptation and compensatory mechanisms in the therapy forecast. Materials and methods: 77 functional slow-transit constipation patients were examined after therapy regimens of functional constipation, the mean age is 44.30±14.58 y.o. Results: The treatment response rates of different therapies with Ipidacrine depends on the patient's initial adaptation and compensatory mechanisms (ACM index); certain aspects allowing to predict the expected result depending on the current mental state were identified; the severity of the state of functional constipation, ACM index and MMPI test psychometric indicators are correlated; adaptation and compensatory mechanisms of functional constipation patients were found to be reduced; the prognosis of the treatment response rates and, accordingly, the choice of the therapy regimen depend on the patient's adaptation potential (index). Conclusion: Therapy regimens for functional constipation patients should be selected on the basis of the original ACM index, behavioral pattern, degree of compliance and the patient's age.

EFFECTIVENESS OF ALPHA-LIPOIC ACID AND Ipidacrine HYDROCHLORIDE IN PREVENTION OF PACLITAXEL-INDUCED PERIPHERAL NEUROPATHY ASSESSED BY ELECTRONEUROMYOGRAPHY OF SUPERFICIAL PERONEAL AND SURAL NERVES

Exp Oncol 2022 Dec;44(4):300-306.PMID:36811539DOI:10.32471/exp-oncology.2312-8852.vol-44-no-4.19030.

Aim: To investigate the neurofunctional parameters in breast cancer (BC) patients with paclitaxel-induced peripheral neuropathy (PIPN) and to clarify the feasibility of using alpha-lipoic acid (ALA) in combination with the acetylcholinesterase inhibitor Ipidacrine hydrochloride (IPD) for its prevention. Materials and methods: 100 BC patients (T1-4N0-3M0-1) prescribed for polychemotherapy (PCT) by the AT (paclitaxel, doxorubicin) or ET (paclitaxel, epirubicin) regimens in the neoadjuvant, adjuvant or palliative modes, were enrolled. The patients were randomized into two groups (n = 50 per group): group I treated by PCT only; group II treated with PCT plus the studied PIPN prevention scheme (ALA in combination with IPD). An electroneuromyography (ENMG) of the sensory (superficial peroneal and sural) nerves was performed before PCT, and after the 3 and 6 PCT cycles. Results: According to ENMG data, the electrophysiological disturbances in the sensory nerves were manifested in the form of axonal sensory peripheral neuropathy of a symmetrical nature, which was reflected in a decrease in the amplitude of the action potential (AP) of the studied nerves. The AP reduction in sensory nerves was dominant, in contrast to the nerve conduction velocity, which in most patients remained within the reference values, thus evidencing on axonal degeneration rather than demyelination as an underlying cause of PIPN. The ENMG testing of the sensory nerve in the groups of BC patients treated by PCT with paclitaxel with or without PIPN prevention treatment established that the use of ALA in combination with IPD significantly improved AP amplitude, duration and area of ​​the response to the stimulation of the superficial peroneal and sural nerves after 3 and 6 PCT cycles. Conclusion: The use of ALA in combination with IPD significantly reduced the severity of damage to the superficial peroneal and sural nerves caused by PCT with paclitaxel and could be recommended for PIPN prevention.

3-(2,3,5,6,7,8-Hexahydro-1H-cyclo-penta-[b]quinolin-9-yl)-1,5-bis-(4-methoxy-phen-yl)biuret

Acta Crystallogr Sect E Struct Rep Online 2010 Feb 20;66(Pt 3):o655.PMID:21580406DOI:10.1107/S1600536810006057.

Ipidacrine (2,3,5,6,7,8-hexa-hydro-1H-cyclo-penta-[b]quinolin-9-amine) was reacted with 4-methoxy-phenyl isocyanate to give the title compound, C(28)H(30)N(4)O(4). An intra-molecular N-H⋯O hydrogen bond results in an essentially planar [r.m.s. deviation from the mean plane is 0.126 (1) Å] conformation for the biuret unit. The central ring of the quinoline unit is twisted by 78.2 (1)° with respect to the biuret mean plane, whereas the two 4-methoxy-benzene rings are twisted out of this plane by 24.3 (1)° and 48.5 (1)°, resulting in an overall propeller-like structure. An inter-molecular N-H⋯N hydrogen bond between the biuret NH atom and the quinoline ring nitro-gen defines the crystal packing.