同义名 :	PD 123319 (trifluoroacetate salt)
	CAS号 :	136676-91-0
	货号 :	A424325
	分子式 :	C35H34F6N4O7
	纯度 :	99%+
	分子量 :	736.66
	MDL号 :	MFCD08276969
	存储条件：	Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

PD 123319 (Ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM[2]. Anaesthetised and ventilated SHR (spontaneously hypertensive rats) were given PD 123319, 0. 36 mg/kg/min, intravenously, and compared with a control group. PD 123319 did not influence baseline CBF (cerebral blood flow), but resulted in a minor BP (blood pressure) decrease[3]. Further, 125I-All specifically labeled two classes of binding sites for All in a membrane preparation of bovine adrenal glomerulosa cells. PD-123319 did not have any effect on 125I-All binding to this site. The second class of binding sites was more sensitive to PD-123319, with an IC50 of 6. 9 +/- 3. 7 nM, and had a much lower affinity for DuP-753 (IC50 around 10 mM)[4].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.36mL 0.27mL 0.14mL	6.79mL 1.36mL 0.68mL	13.57mL 2.71mL 1.36mL

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]Blankley CJ, Hodges JC, Klutchko SR, Himmelsbach RJ, Chucholowski A, Connolly CJ, Neergaard SJ, Van Nieuwenhze MS, Sebastian A, Quin J 3rd, 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. [3]Estrup TM, Paulson OB, Strandgaard S. 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]Boulay G, Servant G, Luong TT, Escher E, Guillemette G. 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.