N-((1-(2-(tert-ButylaMino)-2-oxoethyl)piperidin-4-yl)Methyl)-3-chloro-5-fluorobenzaMide

Name: N-((1-(2-(tert-ButylaMino)-2-oxoethyl)piperidin-4-yl)Methyl)-3-chloro-5-fluorobenzaMide
SKU: ACM1199236640
Rating: 5 (1 reviews)

CAS

1199236-64-0

Catalog Number

ACM1199236640

Category

Main Products

Molecular Weight

384.00

Molecular Formula

C19H27ClFN3O2

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Specification

Synonyms

4-[[(3-Chloro-5-Fluorobenzoyl)Amino]Methyl]-N-(1,1-Dimethylethyl)-1-Piperidineacetamide

Melting Point

122-124 °C

Appearance

White Solid

Analgesic Mechanism of T-type Calcium Channel Antagonist Z944

Harding E K, et al. British Journal of Pharmacology, 2021, 178(17), 3517-3532.

Z944 is a CNS-penetrant high-affinity T-type calcium channel antagonist. This work evaluates the mechanism of action and efficacy of Z944 as a potential new pain treatment. The study's findings indicate that T-type calcium channels play a crucial role in regulating the activity of layer I pain-processing neurons. Blocking these channels with the clinical-stage drug Z944 has been shown to successfully alleviate pain sensitivity in both male and female subjects.
Experimental methods and results
· In this study, Z944 was used in various experiments to observe how it affects the excitability of layer I neurons and inflammatory pain behavior.
· The findings from voltage-clamp recordings of lamina I spinal neurons in adult rats showed that around 80% of these neurons have a low threshold T-type current, which was effectively blocked by Z944. The prevalent T-type current allowed Z944 to block calcium transients in both somatic and dendritic regions of lamina I neurons evoked by action potentials.
· Additionally, when Z944 was applied to spinal cord slices, it reduced the firing rates of action potentials in a majority of laminae I/II neurons. Furthermore, when Z944 was injected intraperitoneally in doses ranging from 1-10 mg·kg-1, it was able to dose-dependently reverse mechanical allodynia in a model of persistent inflammatory pain induced by complete Freund's adjuvant. Interestingly, both male and female rats experienced similar levels of pain relief and at similar rates after receiving Z944.

Study on the Ameliorative Effect of T-Type Calcium Channel Antagonist Z944 on Epilepsy

Casillas-Espinosa P M, et al. Progress in Neurobiology, 2019, 182, 101677.

This work evaluated the disease-modifying antiepileptic effect of the T-type Ca2+ channel antagonist Z944 on the rat temporal lobe epilepsy (TLE) model after kainic acid (KA)-induced status epilepticus (SE). The results showed that Z944 treatment had a disease-modifying effect on the post-SE model of TLE, reducing epileptic seizures and concurrent depressive-like behaviors and cognitive impairments.
Disease-modifying effects of Z944 for epilepsy
· Z944 administration for 7 days showed good tolerability, with mild and temporary neurological side effects observed in animals receiving both Z944 and levetiracetam compared to those given the vehicle alone.
· The chronic infusion of Z944 for 4 weeks resulted in a significant reduction in the severity and frequency of seizures. Treatment with Z944 following status epilepticus notably decreased the number of seizures per day, demonstrating a significant difference from animals treated with the vehicle or levetiracetam.
· Z944 treatment has been shown to have a positive impact on disease progression by reducing spontaneous recurrent seizures, depressive-like behavior, and cognitive impairments in post-status epilepticus animals.
· Additionally, Z944 treatment following status epilepticus led to a decrease in T-type Ca2+ channel expression in the hippocampus.

What is the molecular formula of ulixacaltamide?

The molecular formula of ulixacaltamide is C19H27ClFN3O2.

What is the molecular weight of ulixacaltamide?

The molecular weight of ulixacaltamide is 383.9 g/mol.

What is the IUPAC name of ulixacaltamide?

The IUPAC name of ulixacaltamide is N-[[1-[2-(tert-butylamino)-2-oxoethyl]piperidin-4-yl]methyl]-3-chloro-5-fluorobenzamide.

What is the InChI of ulixacaltamide?

The InChI of ulixacaltamide is InChI=1S/C19H27ClFN3O2/c1-19(2,3)23-17(25)12-24-6-4-13(5-7-24)11-22-18(26)14-8-15(20)10-16(21)9-14/h8-10,13H,4-7,11-12H2,1-3H3,(H,22,26)(H,23,25).

What is the InChIKey of ulixacaltamide?

The InChIKey of ulixacaltamide is JOCLITFYIMJMNK-UHFFFAOYSA-N.

What is the canonical SMILES of ulixacaltamide?

The canonical SMILES of ulixacaltamide is CC(C)(C)NC(=O)CN1CCC(CC1)CNC(=O)C2=CC(=CC(=C2)Cl)F.

What is the CAS number of ulixacaltamide?

The CAS number of ulixacaltamide is 1199236-64-0.

What is the UNII of ulixacaltamide?

The UNII of ulixacaltamide is QT2PJH89C3.

What is the XLogP3-AA value of ulixacaltamide?

The XLogP3-AA value of ulixacaltamide is 3.

What is the topological polar surface area of ulixacaltamide?

The topological polar surface area of ulixacaltamide is 61.4Å².