CV 1808

Names

[ Name ]:
CV 1808

[Synonym ]:
[3H]-2-Phenylaminoadenosine

Biological Activity

[Description]:

CV1808 (2-Phenylaminoadenosine) is a non-selective A2 adenosine receptor (A2 AR) agonist with Kis of 76 and 1450 nM for A2A and A3 adenosine receptor subtypes, respectively[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[Target]

Human Endogenous Metabolite

[In Vitro]

CV1808 demonstrates an inhibitory effect on anti-IgE-induced activation at 100 μM[1]. In the presence of Forskolin (1 μM in PC12 cells; 10 μM in Jurkat cells) the EC50 value for CV1808 is 2 μM[2].

[In Vivo]

Single afferent arterioles of Sprague-Dawley rats are visualized and superfused with solutions containing CV1808 (CV-1808). Superfusion with CV1808 (0.002-2 μM) dilates afferent arterioles[3]. Animal Model: Male Sprague-Dawley rat, weighing 370-410 g[3] Dosage: 0.002, 0.02, 0.2, and 2 μM Administration: Single afferent arterioles of Sprague-Dawley rats were visualized and superfused with solutions containing CV-1808 Result: Afferent arteriolar diameter increased from 17.0±0.3 to 17.2±0.4, 17.8±0.4, 18.5±0.5, and 19.9±0.7 μM, 17.2±2.4% at concentrations of 0.002, 0.02, 0.2, and 2 μM.

[References]

[1]. K H Yip, et al. Reciprocal modulation of anti-IgE induced histamine release from human mast cells by A₁ and A(2B) adenosine receptors. Br J Pharmacol. 2011 Sep;164(2b):807-19.

[2]. I van der Ploeg,et al.Functional characterization of adenosine A2 receptors in Jurkat cells and PC12 cells using adenosine receptor agonists. Naunyn Schmiedebergs Arch Pharmacol.1996 Feb;353(3):250-60.

[3]. Ming-Guo Feng, et al. Afferent arteriolar vasodilator effect of adenosine predominantly involves adenosine A2B receptor activation. Am J Physiol Renal Physiol. 2010 Aug;299(2):F310-5.

Chemical & Physical Properties

[ Density]:
1.78g/cm3

[ Boiling Point ]:
766ºC at 760mmHg

[ Melting Point ]:
210-212ºC

[ Molecular Formula ]:
C₁₆H₁₈N₆O₄

[ Molecular Weight ]:
358.35

[ Flash Point ]:
417.1ºC

[ Exact Mass ]:
358.13900

[ PSA ]:
151.57000

[ LogP ]:
0.41780

[ Index of Refraction ]:
1.829

[ Storage condition ]:
−20°C

[ Water Solubility ]:
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 3.6 mg/mL

Safety Information

[ WGK Germany ]:
3

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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