Ro 04-6790

Names

[ CAS No. ]:
202466-68-0

[ Name ]:
Ro 04-6790

[Synonym ]:
4-Amino-N-[2,6-bis(methylamino)-4-pyrimidinyl]benzenesulfonamide
4-Amino-N-[2,6-bis(methylamino)-4-pyrimidinyl]benzenesulfonamide dihydrobromide
Benzenesulfonamide, 4-amino-N-[2,6-bis(methylamino)-4-pyrimidinyl]-
4-Amino-N-[2,6-bis(methylamino)pyrimidin-4-yl]benzenesulfonamide
Ro 04-6790
4-amino-N-(2,6-bis-methylaminopyrimidin-4-yl)benzenesulfonamide

Biological Activity

[Description]:

Ro 04-6790 is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors[1].

[Related Catalog]:

Research Areas >> Neurological Disease

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

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

[Target]

Rat 5-HT6 Receptor:7.26 (pKi)

Human 5-HT6 Receptor:7.35 (pKi)

[In Vitro]

Ro 04-6790 has over 100 fold selective for the 5-HT6 receptor compared to other receptor binding sites (IC50>10 μM)[1].

[In Vivo]

Ro 04-6790 (10 mg/kg, SC) produces a modest (50%) increase in ACh outflow in adult male Wistar rats of 250-300 g (this effect is not statistically different from the action of vehicle)[2].

[References]

[1]. A J Sleight, et al. Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors. Br J Pharmacol. 1998 Jun;124(3):556-62.

[2]. Sudabeh Shirazi-Southall, et al. Effects of typical and atypical antipsychotics and receptor selective compounds on acetylcholine efflux in the hippocampus of the rat. Neuropsychopharmacology. 2002 May;26(5):583-94.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
595.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₂H₁₆N₆O₂S

[ Molecular Weight ]:
308.359

[ Flash Point ]:
314.1±32.9 °C

[ Exact Mass ]:
308.105530

[ PSA ]:
130.41000

[ LogP ]:
-0.52

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.700

Safety Information

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
DA9462500

[ HS Code ]:
2935009090

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

Articles

Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.

Br. J. Pharmacol. 124 , 556-562, (1998)

1. This study describes the in vitro characterization of two potent and selective 5-HT6 receptor antagonists at the rat and human recombinant 5-HT6 receptor. 2. In binding assays with [3H]-LSD, 4-amin...

Investigation of stretching behaviour induced by the selective 5-HT6 receptor antagonist, Ro 04-6790, in rats.

Br. J. Pharmacol. 126 , 1537-1542, (1999)

1. The present study examined the effects of the selective 5-HT6 receptor antagonist 4-amino-N-(2, 6 bis-methylamino-pyrimidin-4-yl)-benzene sulphonamide (Ro 04-6790) on locomotor activity and uncondi...