Ro 41-1049 (hydrochloride)

Modify Date: 2024-01-02 19:05:06

Ro 41-1049 (hydrochloride) structure	Common Name	Ro 41-1049 (hydrochloride)
	CAS Number	127917-66-2	Molecular Weight	301.76800
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₂H₁₃ClFN₃OS	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Ro 41-1049 (hydrochloride)

Ro 41-1049 hydrochloride is a selective, reversible, orally-active MAO-A inhibitor.Target: MAOin vivo: Ro 41-1049 is an inhibitor of the enzyme monoamine oxidase type A (MAO-A) to rats and monitored extracellular catecholamine levels in the corpus striatum before and after the intraperitoneal (IP) administration of a bolus of L-dopa. Acute administration of Ro 41-1049 (1-50 mg/kg IP) produced a dose-dependent decrease in basal levels of the dopamine metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) and an increase in basal levels of dopamine. In rats treated with Ro 41-1049 (20 mg/kg IP), L-dopa administration (100 mg/kg IP) produced a greater increase in striatal levels of dopamine than it did in controls, while DOPAC and HVA formation was attenuated. We conclude that inhibition of central MAO-A activity promotes synaptic accumulation of dopamine following administration of pharmacological doses of L-dopa.

Name	N-(2-aminoethyl)-5-(3-fluorophenyl)-1,3-thiazole-4-carboxamide,hydrochloride
Synonym	More Synonyms

Description	Ro 41-1049 hydrochloride is a selective, reversible, orally-active MAO-A inhibitor.Target: MAOin vivo: Ro 41-1049 is an inhibitor of the enzyme monoamine oxidase type A (MAO-A) to rats and monitored extracellular catecholamine levels in the corpus striatum before and after the intraperitoneal (IP) administration of a bolus of L-dopa. Acute administration of Ro 41-1049 (1-50 mg/kg IP) produced a dose-dependent decrease in basal levels of the dopamine metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) and an increase in basal levels of dopamine. In rats treated with Ro 41-1049 (20 mg/kg IP), L-dopa administration (100 mg/kg IP) produced a greater increase in striatal levels of dopamine than it did in controls, while DOPAC and HVA formation was attenuated. We conclude that inhibition of central MAO-A activity promotes synaptic accumulation of dopamine following administration of pharmacological doses of L-dopa.
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase Research Areas >> Neurological Disease
References	[1]. Cesura AM, et al. Characterization of the binding of [3H]Ro 41-1049 to the active site of human monoamine oxidase-A. Mol Pharmacol. 1990 Mar;37(3):358-66. [2]. Richards G, et al. Up-regulation of the isoenzymes MAO-A and MAO-B in the human basal ganglia and pons in Huntington's disease revealed by quantitative enzyme radioautography. Brain Res. 2011 Jan 25;1370:204-14. [3]. Brannan T, et al. Effect of a selective MAO-A inhibitor (Ro 41-1049) on striatal L-dopa and dopamine metabolism: an in vivo study. J Neural Transm Park Dis Dement Sect. 1994;8(1-2):99-105.

Description

Related Catalog

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase

Research Areas >> Neurological Disease

References

[1]. Cesura AM, et al. Characterization of the binding of [3H]Ro 41-1049 to the active site of human monoamine oxidase-A. Mol Pharmacol. 1990 Mar;37(3):358-66.

[2]. Richards G, et al. Up-regulation of the isoenzymes MAO-A and MAO-B in the human basal ganglia and pons in Huntington's disease revealed by quantitative enzyme radioautography. Brain Res. 2011 Jan 25;1370:204-14.

[3]. Brannan T, et al. Effect of a selective MAO-A inhibitor (Ro 41-1049) on striatal L-dopa and dopamine metabolism: an in vivo study. J Neural Transm Park Dis Dement Sect. 1994;8(1-2):99-105.