130663-39-7

• 常用中文名：PD 123319
• 常用英文名：PD 123319
• CAS号：130663-39-7
• 分子式：C₃₁H₃₂N₄O₃
• 分子量：508.61
• 相关类别： 生物化工 抑制剂 内分泌及激素(Endocrinology & Hormones) RAAS 拮抗剂
• 发布时间：2017-03-20 10:55:25
• 更新时间：2026-07-07 09:54:11
• PD 123319是血管紧张素II受体拮抗剂,IC50为34 nM。

名称

• 中文名: PD 123319
• 英文名: pd123319
• 中文别名: (6S)-1-[[4-(二甲氨基)-3-甲基苯基]甲基]-5-(2,2-二苯乙酰基)-4,5,6,7-四氢-1H-咪唑并[4,5-C]吡啶-6-羧酸
• 英文别名: S(+)-1-[[4-(DIMETHYLAMINO)-3-METHYLPHENYL]METHYL]-5-(DIPHENYLACETYL)-4,5,6,7-TETRAHYDRO-1H-IMIDAZOL[4,5-C]PYRIDINE-6-CBOXYLIC ACID DITRIFLUOROACETATE; (S)-1-<<4-(dimethylamino)-3-methylphenyl>methyl>-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo<4,5-c>pyridine-6-carboxylic acid; 1H-Imidazo[4,5-c]pyridine-6-carboxylic acid, 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S)-, compd. with 2,2,2-trifluoroacetic acid (1:2); (3S)-9-[(4-DIMETHYLAMINO-3-METHYL-PHENYL)METHYL]-4-(2,2-DIPHENYLACETYL)-4,7,9-TRIAZABICYCLO[4.3.0]NONA-7,10-DIENE-3-CARBOXYLIC ACID; 1H-Imidazo(4,5-C)pyridine-6-cboxylic acid, 1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-, (S); 1-((4-(Dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4.5-c]pyridine-6-carboxyli; PD 123,319 DITRIFLUOROACETATE; PD 123319 ditrifluor; pd 123,319 di(trifluoroacetate) salt; (S)-(+)-PD; (6S)-1-[[4-(Dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-cboxylic acid; PD-123319 TFA salt; (6S)-1-[4-Dimethylamino-3-methylbenzyl]-5-diphenylacetyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6α-cboxylic acid; PD 123; 1-[[4-(DIMETHYLAMINO)-3-METHYLPHENYL]METHYL]-5-(DIPHENYLACETYL)-4,5,6,7-TETRAHYDRO-1H-IMIDAZO[4,5-C]PYRIDINE-6-CBOXYLIC ACID DITRIFLUOROACETATE; (3S)-9-[(4-DIMETHYLAMINO-3-METHYL-PHENYL)METHYL]-4-(2,2-DIPHENYLACETYL)-4,7,9-TRIAZABICYCLO[4.3.0]NONA-7,10-DIENE-3-CBOXYLIC ACID; (S)-(+)-PD 123319|||PD; 1-[[4-(dimethylamino)-3-methylphenyl]methyl]-5-(2,2-diphenylacetyl)-6,7-dihydro-4H-imidazo[4,5-c]pyridine-6-cboxylic acid; ditrifluoroacetate; (6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid trifluoroacetate (1:2); PD-123319 free base; PD 123319, 10 mM in DMSO; PD 123319 ditrifluoroacetate //BP; PD123319, >=; (6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-cboxylic acid; S-(+)-1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazol(4,5-c)pyridine-6-carboxylic acid; (6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid; PD123319 TFA; (6S)-1-[[4-(Dimethylamino)-3-methylphenyl]methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6α-cboxylic acid; s-(+)-1-[(4-(dimethylamino)-3-methylphenyl)methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1h-imidazo[4,5-c]pyridine-6-cboxylic acid ditrifluoroacetate; PD 123,319; 1H-IMidazo[4,5-c]pyridine-6-cboxylic acid, 1-[[4-(diMethylaMino)-3-Methylphenyl]Methyl]-5-(2,2-diphenylacetyl)-4,5,6,7-tetrahydro-, (6S); PD 123,319 DITRIFLUOROACETATE POTENT AND SELECTIVE; 1-((4-(Dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4.5-c]pyridine-6-cboxyli

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 775.8±60.0 °C at 760 mmHg
• 分子式: C₃₁H₃₂N₄O₃
• 分子量: 508.61
• 闪点: 423.0±32.9 °C
• PSA: 78.67000
• LogP: 4.40
• 外观性状: powder
• 蒸汽压: 0.0±2.8 mmHg at 25°C
• 折射率: 1.641
• 储存条件: 2-8°C
• 水溶解性: H2O: 12 mg/mL

生物活性

• 描述: PD 123319是血管紧张素II受体拮抗剂,IC50为34 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管紧张素受体
  研究领域 >> 心血管疾病
• 靶点:

  IC50: 34 nM (AT2 Receptor)[1]

• 体外研究: PD 123319显示出在许多不同组织中区分AII受体的两个亚类。 125I-AII在牛肾上腺肾小球细胞的膜制剂中特异性标记AII的两类结合位点。第一类(DuP-753敏感)代表AII总结合位点的约85％,并且对DuP-753具有高亲和力(IC50为92.9nM)。 PD-123319对125I-AII与该位点的结合没有任何影响。第二类结合位点对PD-123319更敏感,IC50为6.9 nM,对DuP-753的亲和力低得多(IC50约为10 microM)[2]。
• 动物实验: 在16 SHR中研究了CBF自动调节的下限。 8只动物接受PD 123319，而8只作为对照。静脉内施用PD123319或盐水，并且在注射后和开始自动调节研究之前使BP稳定10分钟。随后通过将血液抽入注射器诱导出血性低血压。通过这种方式，BP逐步降低到可获得的最低水平。在整个研究中，CBF的测量间隔为10至15 mmHg。
• 参考文献:

  [1]. Blankley CJ, et al. Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. J Med Chem. 1991 Nov;34(11):3248-60.

  [2]. Boulay G, et al. Modulation of angiotensin II binding affinity by allosteric interaction of polyvinyl sulfate with an intracellular domain of the DuP-753-sensitive angiotensin II receptor of bovine adrenal glomerulosa. Mol Pharmacol. 1992 Apr;41(4):809-15

  [3]. Estrup TM, et al. No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. J Renin Angiotensin Aldosterone Syst. 2001 Sep;2(3):188-92.

  [4]. Brillante DG, et al. Effects of intravenous PD 123319 on haemodynamic and arterial stiffness indices in healthy volunteers. J Renin Angiotensin Aldosterone Syst. 2005 Sep;6(2):102-6.

安全

• 危害码 (欧洲): Xi
• 风险声明 (欧洲): 36/37/38
• 安全声明 (欧洲): 26
• WGK德国: 3