PD123319 di(trifluoroacetate)

Names

[ Name ]:
PD123319 di(trifluoroacetate)

[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)
S-(+)-1-[(4-(dimethylamino)-3-methylphenyl)methyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid di(trifluoroacetate)
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 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
(S)-1-((4-(dimethylamino)-3-methylphenyl)methyl)-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo(4,5-c)pyridine-6-carboxylic acid,difluoroacetate salt
(6S)-1-[4-(Dimethylamino)-3-methylbenzyl]-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid
(S)-1-{[4-(dimethylamino)-3-methylphenyl]methyl}-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acid
PD 123,319
(S)-1-{[4-(dimethylamino)-3-methylphenyl]methyl}-5-(diphenylacetyl)-4,5,6,7-tetrahydro-1H-imidazo-[4,5-c]pyridine-6-carboxylic acid,ditrifluoroacetate,dihydrate
PD 123319 (ditrifluoroacetate)

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].

[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]

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₅H₃₄F₆N₄O₇

[ Molecular Weight ]:
736.657

[ Exact Mass ]:
736.233154

[ PSA ]:
115.97000

[ LogP ]:
5.04700

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ RIDADR ]:
NONH for all modes of transport

Articles

Contractility of placental vascular smooth muscle cells in response to stimuli produced by the placenta: roles of ACE vs. non-ACE and AT1 vs. AT2 in placental vessel cells.

Placenta 29(6) , 503-9, (2008)

Our previously published work has shown that non-ACE angiotensin II (Ang II) generating system is dominate in the placenta and may play a critical role in regulation of placental vascular contractile ...

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. 41 , 809-815, (1992)

Angiotensin II (AII) is an important regulator of aldosterone secretion by adrenal glomerulosa cells. All interacts with a specific receptor coupled to a guanine nucleotide-binding protein that contro...

Differential blockade of central effects of angiotensin II by AT2-receptor antagonists.

Am. J. Physiol. 265 , H226, (1993)

In conscious, chronically instrumented, male Long-Evans rats, we showed previously that central administration (intracerebroventricular) of the AT1-receptor antagonist EXP-3174 (1 microgram) caused a ...