3-Benzamides and 3,4,5-trimethoxyphenyl amines as calcium channel blockers
| Autor: | Hyewhon Rhim, Bohee Kang, Tae Young Yune, Jung Ae Oh, Jee Youn Lee, Hea-Young Park Choo |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Male
Patch-Clamp Techniques medicine.medical_treatment Clinical Biochemistry Analgesic Pharmaceutical Science Pharmacology Lamotrigine Motor Activity Biochemistry Rats Sprague-Dawley Calcium Channels T-Type Structure-Activity Relationship Calcium Channels N-Type Drug Discovery medicine Animals Humans Amines Molecular Biology Spinal Cord Injuries Voltage-dependent calcium channel Chemistry Calcium channel Organic Chemistry Carbamazepine Calcium Channel Blockers Rats Disease Models Animal Allodynia Anticonvulsant HEK293 Cells Neuropathic pain Molecular Medicine Neuralgia medicine.symptom medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry. 23(18) |
| ISSN: | 1464-3391 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect