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PD 123319

Names

[ CAS No. ]:
130663-39-7

[ Name ]:
PD 123319

[Synonym ]:
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)-
(S)-1-<<4-(dimethylamino)-3-methylphenyl>methyl>-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo<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 trifluoroacetate (1:2)
(6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-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
1-((4-(Dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4.5-c]pyridine-6-carboxyli
PD 123,319
PD 123,319 DITRIFLUOROACETATE
pd 123,319 di(trifluoroacetate) salt
1H-Imidazo(4,5-c)pyridine-6-carboxylic acid, 1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-, (S)-
S-(+)-1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazol(4,5-c)pyridine-6-carboxylic acid
PD 123319

Biological Activity

[Description]:

PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor
Research Areas >> Cardiovascular Disease

[Target]

IC50: 34 nM (AT2 Receptor)[1]


[In Vitro]

PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. 125I-AII specifically label two classes of binding sites for AII in a membrane preparation of bovine adrenal glomerulosa cells. The first class (DuP-753 sensitive) represents approximately 85% of the total binding sites for AII and possesses a high affinity (IC50 of 92.9 nM) for DuP-753. PD-123319 does not have any effect on 125I-AII binding to this site. The second class of binding sites is more sensitive to PD-123319, with an IC50 of 6.9 nM, and has a much lower affinity for DuP-753 (IC50 around 10 microM)[2]. 

[Animal admin]

The lower limit of CBF autoregulation is studied in 16 SHR. Eight animals receive PD 123319, while eight serve as controls. PD 123319 or saline is administered intravenously, and the BP is allowed to stabilise for 10 minutes after the injection and prior to the commencement of the autoregulation study. Haemorrhagic hypotension is subsequently induced by withdrawing blood into a syringe. By this means, BP is reduced stepwise to the lowest obtainable level. Throughout the study, CBF is measured at 10 to 15 mmHg BP intervals.

[References]

[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.


[Related Small Molecules]

Angiotensin II acetate salt | AVE 0991 | A 779 | Tranilast | PD123319 di(trifluoroacetate) | Telmisartan | Angiotensin II Receptor Ligand | Sacubitril/valsartan (LCZ696) | EMA401 | Fimasartan | (Val5)-Angiotensin II | RE 201 | C-Type Natriuretic Peptide (32-53) (human, porcine, rat) acetate salt

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
775.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H32N4O3

[ Molecular Weight ]:
508.61

[ Flash Point ]:
423.0±32.9 °C

[ PSA ]:
78.67000

[ LogP ]:
4.40

[ Appearance of Characters ]:
powder

[ Vapour Pressure ]:
0.0±2.8 mmHg at 25°C

[ Index of Refraction ]:
1.641

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
H2O: 12 mg/mL

Safety Information

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26

[ WGK Germany ]:
3

Related Compounds