Xaliproden hydrochloride

[Description]:

Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases[1][2][3].

[Related Catalog]:

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

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1A Receptor:3 nM (IC50)

D2 Receptor:0.1-1 μM (IC50)

[References]

[1]. Cervo L, et, al. Potential antidepressant properties of SR 57746A, a novel compound with selectivity and high affinity for 5-HT1A receptors. Eur J Pharmacol. 1994 Feb 21; 253(1-2): 139-47.

[2]. Simiand J, et, al. Neuropsychopharmacological profile in rodents of SR 57746A, a new, potent 5-HT1A receptor agonist. Fundam Clin Pharmacol. 1993;7(8):413-27.

[3]. Fournier J, et, al. Protective effects of SR 57746A in central and peripheral models of neurodegenerative disorders in rodents and primates. Neuroscience. 1993 Aug; 55(3): 629-41.

[ Boiling Point ]:
487.8ºC at 760mmHg

[ Molecular Formula ]:
C₂₄H₂₃ClF₃N

[ Molecular Weight ]:
417.89400

[ Flash Point ]:
248.8ºC

[ Exact Mass ]:
417.14700

[ PSA ]:
3.24000

[ LogP ]:
6.93030

Click to get detail MSDS

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xn

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
UT8405666

5-HT1A receptors are involved in the effects of xaliproden on G-protein activation, neurotransmitter release and nociception.

Br. J. Pharmacol. 158(1) , 232-42, (2009)

Xaliproden (SR57746A) is a 5-HT(1A) receptor agonist and neurotrophic agent that reduces oxaliplatin-mediated neuropathy in clinical trials. The present study investigated its profile on in vitro tran...

Magnetic resonance imaging of the neuroprotective effect of xaliproden in rats.

Invest. Radiol. 37(6) , 321-7, (2002)

The neurotrophic effect of Xaliproden has been followed using sequential cerebral magnetic resonance imaging (MRI) in rats with vincristine-induced brain lesion as a model of Alzheimer disease.Ninetee...

The neuroprotective agent SR 57746A abrogates experimental autoimmune encephalomyelitis and impairs associated blood-brain barrier disruption: implications for multiple sclerosis treatment.

Proc. Natl. Acad. Sci. U. S. A. 96(22) , 12855-9, (1999)

Experimental autoimmune encephalomyelitis (EAE) is a T cell autoimmune disorder that is a widely used animal model for multiple sclerosis (MS) and, as in MS, clinical signs of EAE are associated with ...

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