BMY 7378 |
| رقم الكتالوجGC10848 |
BMY 7378 هو مضاد انتقائي لمستقبل الأدرينالية α1D (α1D-AR)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 21102-95-4
Sample solution is provided at 25 µL, 10mM.
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BMY 7378 is a selective antagonist of α1D-adrenergic receptor (α1D-AR) with a pki value of 8.89. It is also a mixed agonist and antagonist of serotonin 1A receptor (5-HT1A R)[1, 2]. BMY 7378 can inhibit angiotensin converting enzyme and has antihypertensive activity[3].
In vitro, BMY 7378 (10nM, 10μM) treatment of AC01 cells significantly inhibited norepinephrine (NA)-induced inositol [1,4,5] triphosphate (IP3) production[4].
In vivo, oral treatment of spontaneously hypertensive rats (SHR) with BMY 7378 (10mg/kg/day) for 4 weeks significantly reduced the blood pressure of the treated rats, improved cardiac myocyte fibrosis and cardiac hypertrophy, and increased the expression of α1D-AR protein[5]. BMY 7378 (5mg/kg) was administered to adult male hamsters via surgically implanted osmotic minipumps for 28 days, which upregulated the mRNA of 5-HT1A and 5-HT1B receptors in the hamster hypothalamus, downregulated the mRNA of 5-HT1A and monoamine oxidase-A in the brainstem, and altered the behavioral circadian rhythm of the hamsters[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.
| Animal experiment [1]: | |
Animal models | Spontaneously hypertensive rats (SHR) |
Preparation Method | Thirty-week-old spontaneously hypertensive rats (SHR) were treated for 4 weeks with BMY 7378 (10mg/kg per day, p.o.), or captopril (angiotensin-converting enzyme inhibitor, 40mg/kg per day, p.o.) (as a positive control). Blood pressure and cardiac function were measured in vivo, cardiac hypertrophy by histology, and α1D-AR protein expression by immunofluorescence. |
Dosage form | 10mg/kg/day; 4 weeks; p.o. |
Applications | BMY 7378 and captopril decreased blood pressure and improved hemodynamic parameters and cardiac function in treated SHR vs. untreated SHR. Histology showed increased cardiomyocyte size, fibrosis, and left ventricular hypertrophy in SHR hearts. BMY 7378 ameliorated fibrosis and cardiac hypertrophy, but had no effect on cardiomyocyte size in SHR. Effects of BMY 7378 were associated with increased α1D-AR protein expression in SHR. |
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 |
| الذوبان | 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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Quality Control & SDS
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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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