3-Benzamides and 3, 4, 5-trimethoxyphenyl amines as calcium channel blockers. Issue 18 (15th September 2015)

• Record Type: Journal Article
• Authors: Kang, Bohee; Oh, Jung Ae; Lee, Jee Youn; Rhim, Hyewhon; Yune, Tae Young; Park Choo, Hea-Young
• Is Part Of: Bioorganic & medicinal chemistry. Volume 23:Issue 18(2015)
• Page Start: 6166
• Page End: 6172
• Publication Date: 2015-09-15
• Subjects: T- and N-type calcium channels -- Neuropathic pain -- Spinal cord injury; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2015.07.067
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: T- and N-type calcium channels have known for relating to therapy of neuropathic pain which is chronic, debilitating pain state. Neuropathic pain is caused by damage of the somatosensory system. It may be associated with abnormal sensations and pain produced by normally non-painful stimuli (allodynia). Neuropathic pain is very difficult to treat, and only some 40–60% of patients achieve partial relief. For a neuropathic pain therapy, anticonvulsant like Lamotrigine, Carbamazepine and a topical anesthetic such as Lidocaine are used. We synthesized 15 novel amine derivatives and evaluated their activities against T-type and N-type calcium channels by whole-cell patch clamp recording on HEK293 cells. Among the tested compounds, compound10 showed good inhibitory activity for both T-type and N-type calcium channels with the IC50 value of 1.9 μM and 4.3 μM, respectively. Compound10 also showed good analgesic activity on rat spinal cord injury model.