(R)-6-氯-1-苯基-2,3,4,5-四氢-1H-苯并[d]氮杂卓-7,8-二醇氢溴酸

• 常用名: (R)-6-氯-1-苯基-2,3,4,5-四氢-1H-苯并[d]氮杂卓-7,8-二醇氢溴酸
• 英文名: SKF 81297 hydrobromide
• CAS号: 67287-39-2
• 分子量: 370.669
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₁₇BrClNO₂
• 熔点: N/A
• 闪点: N/A

用途

SKF 81297氢溴酸盐是一种有效的选择性多巴胺D1受体激动剂[1]。

名称

• 中文名: (R)-6-氯-1-苯基-2,3,4,5-四氢-1H-苯并[d]氮杂卓-7,8-二醇氢溴酸
• 英文名: (R)-6-Chloro-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrobromide

生物活性

• 描述: SKF 81297氢溴酸盐是一种有效的选择性多巴胺D1受体激动剂[1]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体
  信号通路 >> 神经信号通路 >> 多巴胺受体
  研究领域 >> 神经疾病
• 靶点实验:

  D1 Receptor

• 体内研究: SKF 81297氢溴酸盐(0.05-0.3mg/kg肌注,一次) 刺激 MPTP语言损伤猴子的运动行为[1]。 动物模型：四只雄性恒河猴(猕猴,7.0-11.3 kg)[1]剂量：0.05-0.3 mg/kg给药：肌肉注射(i.m.)一次结果：单侧MPTP损伤的恒河猴旋转行为和右手使用显著增加。
• 参考文献:

  [1]. Vermeulen RJ, et al. The selective dopamine D1 receptor agonist, SKF 81297, stimulates motor behaviour of MPTP-lesioned monkeys. Eur J Pharmacol. 1993 Apr 22;235(1):143-7.

  [2]. Auger ML, et al. Amelioration of cognitive impairments induced by GABA hypofunction in the male rat prefrontal cortex by direct and indirect dopamine D1 agonists SKF-81297 and d-Govadine. Neuropharmacology. 2020 Jan 1;162:107844.

物理化学性质

• 分子式: C₁₆H₁₇BrClNO₂
• 分子量: 370.669
• 精确质量: 369.013123
• PSA: 52.49000
• LogP: 4.31570
• InChIKey: RMIJGBMRNYUZRG-UHFFFAOYSA-N
• SMILES: Br.Oc1cc2c(c(Cl)c1O)CCNCC2c1ccccc1

安全信息

• WGK德国: 3
• 海关编码: 2933990090

海关

• 海关编码: 2933990090
• 中文概述: 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
• Summary: 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：qHTS to identify inhibitors of the New Delhi Metallo-beta-lactamase (NDM): assay vali... 来源：NCGC External Id：adst_MBL_Abs_LOPAC_o1

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Renal vasodilator activity was determined in anesthetized dogs 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL664304

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：Central dopaminergic activity for minimum concentration which produced 500 rotations(... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL794227

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

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英文别名

• R(+)-6-CHLORO-7,8-DIHYDROXY-1-PHENYL-2,3,4,5-TETRAHYDRO-1H-3-BENZAZEPINE HYDROBROMIDE
• 1H-3-Benzazepine-7,8-diol, 6-chloro-2,3,4,5-tetrahydro-1-phenyl-, (1R)-, hydrobromide (1:1)
• R-(+)-SKF-81297 hydrobromide
• (±)-6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide
• 6-Chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol hydrobromide (1:1)
• 6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide
• (1R)-6-Chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol hydrobromide (1:1)
• Metastin (human)
• (R)-6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrobromide
• 1H-3-Benzazepine-7,8-diol, 6-chloro-2,3,4,5-tetrahydro-1-phenyl-, hydrobromide (1:1)
• (+/-)-6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine hydrobromide