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BD 1008 dihydrobromide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BD 1008 dihydrobromide图片
CAS NO:138356-09-9
规格:98%
分子量:463.08
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
δ1-receptor antagonist,potent and selective
CAS:138356-09-9
分子式:C15H22Cl2N2.2HBr
分子量:463.08
纯度:98%
存储:Store at -20°C

Background:

BD 1008 dihydrobromide is a potent and selective ligand for σ-receptor with Ki values of 2 and 8 nM for σ-1 receptor and σ-2 receptor, respectively [1].


σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2 [2].


BD 1008 dihydrobromide is a potent and selective σ-receptor ligand. BD1008 showed high affinity to sites labeled by 4-[125I]PEMP with Ki value of 5.06 nM in guinea pig brain membranes. In MCF-7 breast cancer and melanoma (A375) cells, 4-[125I]PEMP inhibited the binding of BD1008 with Ki value of 11 nM in a dose-dependent way [2]. In Xenopus oocytes coexpressed N-methyl-D-aspartate (NMDA) receptor (NR) 1a with either NR2A, 2B or 2C, BD1008 inhibited NMDA-activated membrane current responses with IC50 values of 62, 18 and 120 μM for NR1a/2A, NR1a/2B and NR1a/2C respectively, which were due to direct effects on the receptor channel complex [3].


In mice, BD1008 (1 mg/kg) inhibited cocaine-induced locomotor activity with ED50 value increased from 6.50 mg/kg to 11.19 mg/kg [1].


参考文献:
[1].  McCracken KA, Bowen WD, Matsumoto RR. Novel sigma receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur J Pharmacol, 1999, 365(1): 35-38.
[2].  John CS, Gulden ME, Vilner BJ, et al. Synthesis, in vitro validation and in vivo pharmacokinetics of [125I]N-[2-(4-iodophenyl)ethyl]-N-methyl-2-(1-piperidinyl) ethylamine: a high-affinity ligand for imaging sigma receptor positive tumors. Nucl Med Biol, 1996, 23(6): 761-766.
[3].  Whittemore ER, Ilyin VI, Woodward RM. Antagonism of N-methyl-D-aspartate receptors by sigma site ligands: potency, subtype-selectivity and mechanisms of inhibition. J Pharmacol Exp Ther, 1997, 282(1): 326-338.