Antibodies
BMY 7378
- 貨號 Cat. No.
- S2691
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
BMY 7378
Catalog No.S2691
BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3. | |||||
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| Targets | α2C-adrenoceptor | α1D-adrenoceptor | ||||
| IC50 | 6.54 (pKi) [1] | 8.2 (pKi) [2] | ||||
| In vitro | BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. [1]BMY 7378 is selective for the α1D-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; rat α1d-adrenoceptor 8.2, human α1d-adrenoceptor 9.4 [2] BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. [3] | |||||
| In vivo | BMY 7378 (pA2 of 8.67) is approximately 100 times more potent than yohimbine (pA2 of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA2 of 6.48) is approximately 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-adrenoceptor).[1] BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats. [4] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Radioligand Binding Assays | Rat kidney membranes and membranes of Sf9 cells expressing human recombinant α2C -adrenoceptors are prepared. The resultant pellets are used immediately or stored at -20 °C for later use.Pellets are reconstituted in 10 volumes (kidney) or 25 volumes (Sf9 cells) of incubation buffer. In saturation experiments, aliquots of membrane suspension are incubated with various concentrations of [3H]-yohimbine (speciï¬c activity: 81 Ci mmol-1) at 25 °C (rat kidney: 0.5-30 nM; Sf9 cells: 0.2-20 nM; rat submandibular gland: 1.0-40 nM; incubation buffer: Tris-HCl 50 mM, EDTA 5 mM, pH 7.4 at 25 °C). In competition studies, [3H]-yohimbine (5 or 10 nM) is incubated with competing ligands in concentrations from 0.1 nM to 1 mM in 0.5 log unit increments for 30 min. Non-speciï¬c binding is determined in the presence of phentolamine (10 lM). Speciï¬c binding of [3H]-yohimbine is 70-90% of total binding at the concentration used in displacement experiments. Assays are terminated by washing with ice-cold incubation buffer, followed by rapid vacuum ï¬ltration through Whatman GF/C ï¬lters, using a Brandel Cell Harvester. Radioactivity retained on ï¬lters is determined by liquid scintillation spectroscopy. |
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Animal Study: [4]
| Animal Models | rats |
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| Dosages | 0.25-5 mg/kg |
| Administration | Inject subcutaneously at a single dose |
| Solubility | Saline, 15 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 458.42 |
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| Formula | C22H31N3O3.2HCl |
| CAS No. | 21102-95-4 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 92 mg/mL (200 mM) |
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| Water | 92 mg/mL (200 mM) | ||
| Ethanol | 20 mg/mL (43 mM) | ||
| In vivo | Saline, | 15 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 8-Azaspiro[4.5]decane-7,9-dione, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-, hydrochloride (1:2) |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.45842 | 4.5842 | 9.1684 | 13.7526 |
