Fenoldopam (mesylate)

Names

[ Name ]:
Fenoldopam (mesylate)

[Synonym ]:
EINECS 266-612-7
Fenoldopam monomethanesulfonate
MFCD04112986
6-Chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-(p-hydroxyphenyl)-1H-3-benzazepinium methanesulphonate
Corlopam
Fenoldopam methanesulfonate
6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzazepine-7,8-diol methanesulfonate
9-chloro-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Fenoldopam mesylate
6-chloro-7,8-dihydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine methanesulfonate
6-chloro-2,3,4,5-tetrahydro-1-(p-hydroxyphenyl)-1H-3-benzazepine-7,8-diol methanesulfonate
CORLOPAM MESYLATE
Fenoldopam (mesylate)

Biological Activity

[Description]:

Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.Target: D1 ReceptorFenoldopam is a selective dopamine-1 (DA1) agonist with natriuretic/diuretic properties. Fenoldopam stimulated cAMP accumulation in LLC-PK1 cells in a dose-dependent manner, an effect which could be blocked by the DA1-selective antagonist Sch 23390. Although fenoldopam was more potent than DA (EC50 55.5 +/- 7.75 nM vs. 1.65 +/- 0.64 microM) in stimulating cAMP accumulation in LLC-PK1 cells, the maximum stimulation obtained by fenoldopam was only 37% of the maximum stimulation obtained by DA(Emax 13.0 +/- 2.95 pmol/mg of protein vs. 35.6 +/- 10.19 pmol/mg of protein) [1]. Fenoldopam is a selective dopamine1 (DA1) receptor agonist. Most of the DA1 receptor agonist activity of fenoldopam resides in the R-enantiomer, which also shows weaker alpha 2-adrenoceptor antagonist activity Fenoldopam produces vasodilation in vascular beds that are rich in vascular DA1 receptors [2].

[Related Catalog]:

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

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Cardiovascular Disease

[References]

[1]. Grenader, A. and D.P. Healy, Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells. J Pharmacol Exp Ther, 1991. 258(1): p. 193-8.

[2]. Nichols, A.J., R.R. Ruffolo, Jr., and D.P. Brooks, The pharmacology of fenoldopam. Am J Hypertens, 1990. 3(6 Pt 2): p. 116S-119S.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.38g/cm3

[ Boiling Point ]:
522.6ºC at 760 mmHg

[ Molecular Formula ]:
C₁₇H₂₀ClNO₆S

[ Molecular Weight ]:
401.86

[ Flash Point ]:
269.9ºC

[ PSA ]:
104.24000

[ LogP ]:
3.77680

[ Storage condition ]:
room temp

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H317-H319

[ Precautionary Statements ]:
P280-P301 + P312 + P330-P305 + P351 + P338

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-36-42/43

[ Safety Phrases ]:
22-26-36/37/39

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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Previously we found that regulation of eNOS is an important part of the pathogenic process of Drug-induced vascular injury (DIVI) for PDE4i. The aims of the current study were to examine the phosphory...

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Oncolytic viruses (OV) have broad potential as an adjuvant for the treatment of solid tumors. The present study addresses the feasibility of clinically applicable drugs to enhance the oncolytic potent...

Contrast-induced nephropathy: protective role of fenoldopam.

Clin. Exp. Pharmacol. Physiol. 39(6) , 497-505, (2012)

1. Contrast-induced nephropathy (CIN) often occurs after contrast media-related procedures and is associated with increased morbidity and mortality. The acute renal failure observed after administrati...