Kang, Bohee Oh, Jung Ae Lee, Jee Youn Rhim, Hyewhon Yune, Tae Young Choo, Hea-Young Park 2024-01-20T06:30:40Z 2024-01-20T06:30:40Z 2021-09-04 2015-09 0968-0896 https://pubs.kist.re.kr/handle/201004/125093 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 mu M and 4.3 mu M, respectively. Compound 10 also showed good analgesic activity on rat spinal cord injury model. (c) 2015 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. 3-Benzamides and 3,4,5-trimethoxyphenyl amines as calcium channel blockers Article 10.1016/j.bmc.2015.07.067 1 Bioorganic and Medicinal Chemistry, v.23, no.18, pp.6166 - 6172 Bioorganic and Medicinal Chemistry 23 18 6166 6172 N scie scopus 000360910000009 2-s2.0-84940787097 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article SPINAL MECHANISMS BLOCKING ACTIVITY SENSORY NEURONS CA2+ CHANNEL RAT MODEL HYPERALGESIA PAIN ZONISAMIDE ALLODYNIA CELLS T- and N-type calcium channels Neuropathic pain Spinal cord injury