BMY 7378 |
| カタログ番号GC10848 |
BMY 7378は、α1D-アドレナリン受容体(α1D-AR)の選択性な拮抗剤であり、pki値は8.89である。また、セロトニン1A受容体(5-HT1A R)の混合作用剤と拮抗剤である。
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Cas No.: 21102-95-4
Sample solution is provided at 25 µL, 10mM.
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BMY 7378は、α1D-アドレナリン受容体(α1D-AR)の選択性な拮抗剤であり、pki値は8.89である。また、セロトニン1A受容体(5-HT1A R)の混合作用剤と拮抗剤である[1, 2]。BMY 7378は、アンジオテンシン変換酵素を阻害でき、抗高血圧活性を持つ[3]。
体外では、AC01細胞をBMY 7378 (10nM、10μM)で処理した結果、ノルアドレナリン（NA）誘発性のイノシトール[1,4,5]三リン酸(IP3)の生産を著しく阻害した[4]。
生体内では、自発高血圧ラット（SHR）にBMY 7378 (10mg/kg/日)を4週間経口投与した結果、処理されたラットの血圧を著しく減らし、心筋細胞線維症と心臓肥大を改善し、α1D-ARタンパク質の発見を増やした[5]。外科的に埋め込まれた浸透圧ミニポンプを通じて、BMY 7378 (5mg/kg)を成体雄のハムスターに28日間投与した結果、ハムスターの視床下部で5-HT1Aと5-HT1B受容体のmRNAを上部制御し、脳幹における5-HT1Aとモノアミン酸化酵素のmRNAを下方制御し、ハムスターの行動概日リズムをも変えた[6]。
References:
[1] Chen J. Characterisation of novel alpha1-adrenoceptor ligands[D]. UNSW Sydney, 2014.
[2] Jeffers R. The Involvement of the Intergeniculate Leaflet in the Potentiation of Photic Phase Shifts by the 5-HT1A Mixed Agonist/Antagonist BMY 7378[J]. 2013.
[3] Rodríguez J E, Andrade-Jorge E, Barquet-Nieto A, et al. BMY 7378, a selective α1D-adrenoceptor antagonist, is a new angiotensin converting enzyme inhibitor: In silico, in vitro and in vivo approach[J]. Biochimica et Biophysica Acta (BBA)-General Subjects, 2025, 1869(1): 130732.
[4] Ohmi K, Shinoura H, Nakayama Y, et al. Characterization of α1‐adrenoceptors expressed in a novel vascular smooth muscle cell line cloned from p53 knockout mice, P53LMAC01 (AC01) cells[J]. British journal of pharmacology, 1999, 127(3): 756-762.
[5] Rodríguez J E, Saucedo-Campos A D, Vega A V, et al. The α1D-adrenoreceptor antagonist BMY 7378 reverses cardiac hypertrophy in spontaneously hypertensive rats[J]. Journal of Hypertension, 2020, 38(8): 1496-1503.
[6] Vijaya Shankara J, Orr A, Mychasiuk R, et al. Chronic BMY 7378 treatment alters behavioral circadian rhythms[J]. European Journal of Neuroscience, 2017, 46(11): 2782-2790.
| 動物実験 [1]: | |
動物モデル | 自発性高血圧ラット（SHR） |
準備方法 | 30週齢の自発性高血圧ラット（SHR）を、BMY 7378 (10mg/kg/日、経口)またはカプトリル（アンジオテンシン変換酵素阻害剤、40mg/kg/日、経口）（陽性対照物として）で4週間処理した。血圧と心臓機能を生体内で測定し、心臓肥大を組織学的に測定し、α1D-ARタンパク質の発見を免疫蛍光染色で測定した。 |
投与形態 | 10mg/kg/日；4週間；経口 |
アプリケーション | BMY 7378とカプトリルは、投与されたSHRは未投与のSHRに比べて、血圧を減らし、血行動態パラメーターと心臓機能を改善した。組織学的な検査の結果、SHRの心臓では、心筋サイズ、線維化と左室肥大が観察された。BMY 7378は線維症と心臓肥大を改善したが、SHRにおける心筋のサイズには影響がなかった。BMY 7378の効果は、SHRにおけるα1D-ARタンパク質の発見の増加と関連していた。 |
References: | |
| Cas No. | 21102-95-4 | SDF | |
| Chemical Name | 8-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-8-azaspiro[4.5]decane-7,9-dione;dihydrochloride | ||
| Canonical SMILES | COC1=CC=CC=C1N2CCN(CC2)CCN3C(=O)CC4(CCCC4)CC3=O.Cl.Cl | ||
| Formula | C22H31N3O3.2HCl | M.Wt | 458.42 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 25 mg/ml,Ethanol: 0.2 mg/ml,PBS (pH 7.2): 0.5 mg/ml | 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. |
||
| 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 | 2.1814 mL | 10.907 mL | 21.8141 mL |
| 5 mM | 436.3 μL | 2.1814 mL | 4.3628 mL |
| 10 mM | 218.1 μL | 1.0907 mL | 2.1814 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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