(+)-Dihydrexidine hydrochloride
(Synonyms: (+)-DAR-0100 hydrochloride) 目录号 : GC17527(+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) 是一种多巴胺 D1 受体激动剂,EC50 为 72± 21 nM。
Cas No.:158704-02-0
Sample solution is provided at 25 µL, 10mM.
(+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
(+)-Dihydrexidine hydrochloride (DHX) is a high-potency, bioavailable D1 dopamine receptor agonist. (+)-Dihydrexidine is screened for activity against 40 other binding sites, and is inactive (IC50 greater than 10 microM) against all except D2 dopamine receptors (IC50=130 nM) and alpha 2 adrenoreceptors (IC50=230 nM). Dihydrexidine competes stereoselectively and potently for D1 binding sites in rat striatal membranes labeled with [3H]SCH23390 with an IC50 of about 10 nM compared to about 30 nM for the prototypical D1 agonist SKF38393[2].
To examine the functional state of striatal neurons in response to D1 receptor activation, AC5+/+ and AC5-/- mice are injected with the D1 agonist (+)-Dihydrexidine (30 mg/kg, i.p.) and obtained the dorso-lateral striatum and NAc, separately, 45 min later for RT-PCR analysis. These experiments reveal that (+)-Dihydrexidine -triggered induction of the immediate early genes, c-fos, egr-1, and junB, in the NAc is markedly enhanced in AC5-/- mice compared with that in AC5+/+ mice, while the induction in the dorso-lateral striatum is suppressed in AC5-/- mice[3].
References:
[1]. Lewis MM, et al. Homologous desensitization of the D1A dopamine receptor: efficacy in causing desensitizationdissociates from both receptor occupancy and functional potency. J Pharmacol Exp Ther. 1998 Jul;286(1):345-53.
[2]. Mottola DM, et al. Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. J Pharmacol Exp Ther. 1992 Jul;262(1):383-93.
[3]. Kim KS, et al. Adenylyl cyclase-5 activity in the nucleus accumbens regulates anxiety-related behavior. J Neurochem. 2008 Oct;107(1):105-15.
Animal experiment: | Mice[3]AC5-/- mice are backcrossed to the C57BL/6J strain for 9 or 10 generations to obtain heterozygote N9 or N10 mice. Mice are treated with (+)-Dihydrexidine (30 mg/kg, i.p.)[3]. |
References: [1]. Lewis MM, et al. Homologous desensitization of the D1A dopamine receptor: efficacy in causing desensitizationdissociates from both receptor occupancy and functional potency. J Pharmacol Exp Ther. 1998 Jul;286(1):345-53. |
Cas No. | 158704-02-0 | SDF | |
别名 | (+)-DAR-0100 hydrochloride | ||
化学名 | (6aR,12bS)-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine-10,11-diol hydrochloride | ||
Canonical SMILES | OC(C=C1[C@@H]2[C@@H](CCC1=C3)NCC4=CC=CC=C24)=C3O.Cl | ||
分子式 | C17H17NO2.HCl | 分子量 | 303.79 |
溶解度 | <15.19mg/ml in DMSO | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.2917 mL | 16.4587 mL | 32.9175 mL |
5 mM | 0.6583 mL | 3.2917 mL | 6.5835 mL |
10 mM | 0.3292 mL | 1.6459 mL | 3.2917 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
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