BU 239 hydrochloride
目录号 : GC11580
Imidazoline receptors-selective antagonist
Cas No.:1217041-98-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Target: I1 imidazoline receptor, I2 imidazoline receptor
IC50: 35 nM, 47 nM
BU 239 hydrochloride is an imidazoline receptors-selective antagonist. BU239 displayed high affinity for both I1 imidazoline and I2 imidazoline receptors in competition binding experiments with IC50 values of 35 nM and 47 nM, respectively [1]. The imidazoline receptors involved in circulatory system are classified in two groups: the I1 type and the I2 type. I1 type is sensitive to idazoxan and clonidine, an antagonist with an imidazoline structure. I2 type displays a high affinity for idazoxan, cirazoline, guanabenz and a medium-tolow affinity for clonidine. In particular, Imidazoline I1 receptors play a critical role in the central regulation of blood pressure [2].
In vitro: BU239 (1 μM) reversed α2 agonists-mediated inhibition of arginine vasopressin (AVP)-stimulated water permeability in the rat inner medullary collecting duct (IMCD) [3]. In addition, BU239 significantly reversed agmatine-induced inhibition of AVP-stimulated urea permeability (Pu) in IMCD [4]. BU239 produced positive inotropic activity with the maximum effect observed at 117.4 % [2].
In vivo: N/A
References:
1. Flamez A, De Backer JP, Czerwiec E, Ladure P, Vauquelin G. Pharmacological characterization of I1 and I2 imidazoline receptors in human striatum. Neurochem Int. 1997;30(1):25-9.
2. Radwanska A, Dlugokecka J, Wasilewski R, Kaliszan R. Testing conception of engagement of imidazoline receptors in imidazoline drugs effects on isolated rat heart atria. J Physiol Pharmacol. 2009;60(1):131-42.
3. Kudo LH, Hebert CA, Rouch AJ. Inhibition of water permeability in the rat collecting duct: effect of imidazoline and alpha-2 compounds. Proc Soc Exp Biol Med. 1999;221(2):136-46.
4. Rouch AJ, Kudo LH. Agmatine inhibits arginine vasopressin-stimulated urea transport in the rat inner medullary collecting duct. Kidney Int. 2002;62(6):2101-8.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2609 mL | 21.3047 mL | 42.6094 mL |
| 5 mM | 0.8522 mL | 4.2609 mL | 8.5219 mL |
| 10 mM | 0.4261 mL | 2.1305 mL | 4.2609 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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