title: 3-Benzamides and 3,4,5-trimethoxyphenyl amines as calcium channel blockers.
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, compound 10 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. Compound 10 also showed good analgesic activity on rat spinal cord injury model.
authors: College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors: Bohee
authors: B
authors: Kang
authors: College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors: Jung Ae
authors: JA
authors: Oh
authors: Age-Related and Brain Diseases Research Center, Kyunghee University, Seoul, Republic of Korea.
authors: Jee Youn
authors: JY
authors: Lee
authors: Center for Neuroscience, Korea Institute of Science & Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
authors: Hyewhon
authors: H
authors: Rhim
authors: Department of Biochemistry, Kyunghee University School of Medicine, Seoul, Republic of Korea. Electronic address: tyune@khu.ac.kr.
authors: Tae Young
authors: TY
authors: Yune
authors: College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea. Electronic address: hypark@ewha.ac.kr.
authors: Hea-Young
authors: HY
authors: Park Choo
mesh_terms: D000588:Amines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D020864:Calcium Channels, N-Type / Q000737:chemistry / Q000378:metabolism; D020747:Calcium Channels, T-Type / Q000737:chemistry / Q000378:metabolism; D004195:Disease Models, Animal; D057809:HEK293 Cells; D006801:Humans; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D009437:Neuralgia / Q000188:drug therapy; D018408:Patch-Clamp Techniques; D051381:Rats; D017207:Rats, Sprague-Dawley; D013119:Spinal Cord Injuries / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000588:Amines; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D020747:Calcium Channels, T-Type
keywords: Neuropathic pain; Spinal cord injury; T- and N-type calcium channels