Agomelatine (Synonyms: S20098) |
| Catalog No.GC17981 |
Agomelatine은 MT1 및 MT2 수용체에 대한 Ki 값이 각각 0.1 nM 및 0.12 nM인 멜라토닌(MT) 수용체 자극제이다. Agomelatine은 또한 5-HT2C 및 5-HT2B에 대한 Ki 값이 각각 631 nM 및 660 nM인 5-hydroxytryptamine (5-HT)수용체 항agonist이다.
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Cas No.: 138112-76-2
Sample solution is provided at 25 µL, 10mM.
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Agomelatine은 MT1 및 MT2 수용체에 대한 Ki 값이 각각 0.1 nM 및 0.12 nM인 멜라토닌(MT) 수용체 자극제이다. Agomelatine은 또한 5-HT2C 및 5-HT2B에 대한 Ki 값이 각각 631 nM 및 660 nM인 5-hydroxytryptamine (5-HT)수용체 항agonist이다.
Agomelatine은 생물리 리듬을 조절하고 기분을 향상시킬 수 있으며, 중증 우울증(MDD) 연구에 사용된다[3].
체외 실험에서 Agomelatine (10, 20 μM)은 24시간 동안 혈관 내피세포와 단핵세포를 처리하여, 복용량에 따라 dose-dependently II-induced증가를 유도하는 AT1R, VCAM-1 및 ICAM-1의 표현 증가를 억제하고, 세포 응집을 감소시켰다[4]. Agomelatine (8, 16 μM)은 24시간 동안 해마 뉴런 HT22 세포를 처리하여, 시스플랫닌 손상으로 인한 신경 독성을 억제하고, 산화 스트레스와 염증 반응을 완화시켰다[5].
체내 실험에서 Agomelatine (40mg/kg)은 복강 주사로 LPS를 유도한 우울증이 있는 쥐에게 치료를 제공하여, 대소의 불안 및 우울증과 같은 행동을 현저하게 개선하고 신경 염증과 뉴런 손상을 감소시켰다[6]. Agomelatine (25, 50 또는 75 mg/kg; 복강 주사)은 쥐 뇌전증 모델에서 항산화 활동을 가지고 있다[7].
References:
[1] Dridi D, Zouiten A, Mansour H B. Depression: chronophysiology and chronotherapy[J]. Biological rhythm research, 2014, 45(1): 77-91.
[2] Millan M J, Gobert A, Lejeune F, et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 306(3): 954-964.
[3] Smeraldi E, Delmonte D. Agomelatine in depression[J]. Expert opinion on drug safety, 2013, 12(6): 873-880.
[4] Hong N, Ye Z, Lin Y, et al. Agomelatine prevents angiotensin II-induced endothelial and mononuclear cell adhesion[J]. Aging (albany NY), 2021, 13(14): 18515.
[5] Cankara F N, Günaydın C, Çelik Z B, et al. Agomelatine confers neuroprotection against cisplatin-induced hippocampal neurotoxicity[J]. Metabolic brain disease, 2021, 36(2): 339-349.
[6] Lan T, Wu Y, Zhang Y, et al. Agomelatine rescues lipopolysaccharide-induced neural injury and depression-like behaviors via suppression of the Gαi-2-PKA-ASK1 signaling pathway[J]. Journal of neuroinflammation, 2022, 19(1): 117.
[7] Aguiar C C T, Almeida A B, Araújo P V P, et al. Effects of agomelatine on oxidative stress in the brain of mice after chemically induced seizures[J]. Cellular and molecular neurobiology, 2013, 33: 825-835.
세포 실험 [1]: | |
세포 라인 | HUVEC 세포 |
제조 방법 | 인간 HUVECs는 Ang II(1μM)에 노출되며, Agomelatine(10, 20 μM)을 추가하거나 추가하지 않고 24시간 처리하였다. |
반응 조건 | 10, 20 μM; 24 h |
응용 분야 | 10 및 20μM Agomelatine의 도입은 Ang II에 대한 노출로 인한 AT1R 표현 증가를 방지했으며, 높은 복용량은 더 강한 억제 효과를 보였다. |
동물 실험 [2]: | |
동물 모형 | LPS 유도된 쥐 우울증 모델 |
제조 방법 | 아고멜라틴은 1% 히드록시에틸 셀룰로스(HEC) 용액에 용해되었다. 모든 실험에서 Agomelatine(40mg/kg)은 일일 LPS 처리 60분 전에 i.p.를 통하여 투여되었다. |
제형 | 40mg/kg; i.p. |
응용 분야 | 아고멜라틴은 LPS가 유도한 쥐의 우울증과 같은 행동을 반전시킬 수 있고, 뇌의 DG 영역에서의 신경염증 반응을 감소시킬 수 있다. |
참고문헌: [1] Hong N, Ye Z, Lin Y, 등. 아고멜라틴은 혈관 긴장소 II 유발의 내피세포 및 단핵세포 붙임을 예방할 수 있다[J]. 연령 (앨버니 NY), 2021, 13(14): 18515. [2] Lan T, Wu Y, Zhang Y, 등. 아고멜라틴은 Gαi-2-PKA-ASK1 신호 전달 경로를 억제하여 LPS 유도된 신경 손상과 우울증과 같은 행동을 구제한다[J]. 뇌염증학, 2022, 19(1): 117. | |
| Cas No. | 138112-76-2 | SDF | |
| Synonyms | S20098 | ||
| Chemical Name | N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide | ||
| Canonical SMILES | CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC | ||
| Formula | C15H17NO2 | M.Wt | 243.3 |
| Solubility | ≥ 12.2mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.1102 mL | 20.5508 mL | 41.1015 mL |
| 5 mM | 0.822 mL | 4.1102 mL | 8.2203 mL |
| 10 mM | 0.411 mL | 2.0551 mL | 4.1102 mL |
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Quality Control & SDS
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- Purity: >98.50%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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