Ro 04-6790 HCl hydrate | CAS#unknown | 5-HT6 antagonist

MedKoo Cat#: 464929 | Name: Ro 04-6790 HCl hydrate

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ro 04-6790 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 44.7 nM).1 It is selective for 5-HT6 receptors over a panel of 23 additional receptors at 10 µM. Ro 04-6790 inhibits 5-HT-induced cAMP production in HeLa cells expressing human 5-HT6 (pA2 = 6.75). In vivo, Ro 04-6790 (10 and 30 mg/kg) induces stretching and yawning behavior in rats. It reverses scopolamine-induced decreases in novel object discrimination in rats.2 Ro 04-6790 (3, 10, and 30 mg/kg) also attenuates cue-induced cocaine-seeking behavior in rats.

Chemical Structure

Ro 04-6790 HCl hydrate

CAS#unknown

Theoretical Analysis

MedKoo Cat#: 464929

Name: Ro 04-6790 HCl hydrate

CAS#: unknown

Chemical Formula: C12H20Cl2N6O3S

Exact Mass: 398.0695

Molecular Weight: 399.29

Elemental Analysis: C, 36.10; H, 5.05; Cl, 17.76; N, 21.05; O, 12.02; S, 8.03

Price and Availability

Size	Price	Availability
5mg	USD 400.00	2 Weeks
10mg	USD 600.00	2 Weeks
25mg	USD 1,050.00	2 Weeks

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Related CAS #

1197333-95-1 (dihydrochloride) 202466-68-0 (free base)

Synonym

Ro 04-6790 HCl hydrate; Ro 046790 HCl hydrate; Ro 04 6790 HCl hydrate; Ro 04-6790 hydrochloride hydrate;

IUPAC/Chemical Name

4-amino-N-(2,6-bis(methylamino)pyrimidin-4-yl)benzenesulfonamide dihydrochloride hydrate

InChi Key

NAXNKMHJJJLURY-UHFFFAOYSA-N

InChi Code

InChI=1S/C12H16N6O2S.2ClH.H2O/c1-14-10-7-11(17-12(15-2)16-10)18-21(19,20)9-5-3-8(13)4-6-9;;;/h3-7H,13H2,1-2H3,(H3,14,15,16,17,18);2*1H;1H2

SMILES Code

O=S(NC1=NC(NC)=NC(NC)=C1)(C2=CC=C(N)C=C2)=O.Cl.Cl.O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

	Solvent	mg/mL	mM
Solubility
	DMSO	15.0	37.57
	Water	5.0	12.52

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 399.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Thur KE, Nelson AJ, Cassaday HJ. Ro 04-6790-induced cognitive enhancement: no effect in trace conditioning and novel object recognition procedures in adult male Wistar rats. Pharmacol Biochem Behav. 2014 Dec;127:42-8. doi: 10.1016/j.pbb.2014.10.006. Epub 2014 Oct 24. PMID: 25450117; PMCID: PMC4258611. 2: Fell MJ, Katner JS, Rasmussen K, Nikolayev A, Kuo MS, Nelson DL, Perry KW, Svensson KA. Typical and atypical antipsychotic drugs increase extracellular histamine levels in the rat medial prefrontal cortex: contribution of histamine h(1) receptor blockade. Front Psychiatry. 2012 May 17;3:49. doi: 10.3389/fpsyt.2012.00049. PMID: 22629251; PMCID: PMC3354526. 3: van Gaalen MM, Schetters D, Schoffelmeer AN, De Vries TJ. 5-HT6 antagonism attenuates cue-induced relapse to cocaine seeking without affecting cocaine reinforcement. Int J Neuropsychopharmacol. 2010 Aug;13(7):961-5. doi: 10.1017/S1461145710000428. Epub 2010 Apr 29. PMID: 20426879. 4: Kendall I, Slotten HA, Codony X, Burgueño J, Pauwels PJ, Vela JM, Fone KC. E-6801, a 5-HT6 receptor agonist, improves recognition memory by combined modulation of cholinergic and glutamatergic neurotransmission in the rat. Psychopharmacology (Berl). 2011 Feb;213(2-3):413-30. doi: 10.1007/s00213-010-1854-3. Epub 2010 Apr 20. PMID: 20405281. 5: Glennon RA, Siripurapu U, Roth BL, Kolanos R, Bondarev ML, Sikazwe D, Lee M, Dukat M. The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs. Curr Top Med Chem. 2010;10(5):579-95. doi: 10.2174/156802610791111542. PMID: 20166945; PMCID: PMC5839515. 6: King MV, Spicer CH, Sleight AJ, Marsden CA, Fone KC. Impact of regional 5-HT depletion on the cognitive enhancing effects of a typical 5-ht(6) receptor antagonist, Ro 04-6790, in the Novel Object Discrimination task. Psychopharmacology (Berl). 2009 Jan;202(1-3):111-23. doi: 10.1007/s00213-008-1334-1. Epub 2008 Oct 7. PMID: 18839151. 7: Fone KC. An update on the role of the 5-hydroxytryptamine6 receptor in cognitive function. Neuropharmacology. 2008 Nov;55(6):1015-22. doi: 10.1016/j.neuropharm.2008.06.061. Epub 2008 Jul 4. PMID: 18655798. 8: Pitsikas N, Zisopoulou S, Pappas I, Sakellaridis N. The selective 5-HT(6) receptor antagonist Ro 04-6790 attenuates psychotomimetic effects of the NMDA receptor antagonist MK-801. Behav Brain Res. 2008 Apr 9;188(2):304-9. doi: 10.1016/j.bbr.2007.11.010. Epub 2007 Nov 21. PMID: 18164078. 9: Meneses A. Do serotonin(1-7) receptors modulate short and long-term memory? Neurobiol Learn Mem. 2007 May;87(4):561-72. doi: 10.1016/j.nlm.2006.12.005. Epub 2007 Jan 16. PMID: 17224282. 10: Romero G, Sánchez E, Pujol M, Pérez P, Codony X, Holenz J, Buschmann H, Pauwels PJ. Efficacy of selective 5-HT6 receptor ligands determined by monitoring 5-HT6 receptor-mediated cAMP signaling pathways. Br J Pharmacol. 2006 Aug;148(8):1133-43. doi: 10.1038/sj.bjp.0706827. Epub 2006 Jul 24. PMID: 16865095; PMCID: PMC1752021. 11: Romero G, Pujol M, Pérez P, Buschmann H, Pauwels PJ. Whole spectrum analysis of ligand efficacy at constitutively active human wild-type and S267K 5-HT6 receptors in HEK-293F cells. J Pharmacol Toxicol Methods. 2007 Mar- Apr;55(2):144-50. doi: 10.1016/j.vascn.2006.04.007. Epub 2006 May 9. PMID: 16769227. 12: King MV, Sleight AJ, Woolley ML, Topham IA, Marsden CA, Fone KC. 5-HT6 receptor antagonists reverse delay-dependent deficits in novel object discrimination by enhancing consolidation--an effect sensitive to NMDA receptor antagonism. Neuropharmacology. 2004 Aug;47(2):195-204. doi: 10.1016/j.neuropharm.2004.03.012. PMID: 15223298. 13: Woolley ML, Marsden CA, Sleight AJ, Fone KC. Reversal of a cholinergic- induced deficit in a rodent model of recognition memory by the selective 5-HT6 receptor antagonist, Ro 04-6790. Psychopharmacology (Berl). 2003 Dec;170(4):358-67. doi: 10.1007/s00213-003-1552-5. Epub 2003 Sep 10. PMID: 13680084. 14: Lindner MD, Hodges DB Jr, Hogan JB, Orie AF, Corsa JA, Barten DM, Polson C, Robertson BJ, Guss VL, Gillman KW, Starrett JE Jr, Gribkoff VK. An assessment of the effects of serotonin 6 (5-HT6) receptor antagonists in rodent models of learning. J Pharmacol Exp Ther. 2003 Nov;307(2):682-91. doi: 10.1124/jpet.103.056002. Epub 2003 Sep 15. PMID: 12975483. 15: Leng A, Ouagazzal A, Feldon J, Higgins GA. Effect of the 5-HT6 receptor antagonists Ro04-6790 and Ro65-7199 on latent inhibition and prepulse inhibition in the rat: comparison to clozapine. Pharmacol Biochem Behav. 2003 May;75(2):281-8. doi: 10.1016/s0091-3057(03)00082-0. PMID: 12873617. 16: Meneses A. Role of 5-HT6 receptors in memory formation. Drug News Perspect. 2001 Sep;14(7):396-400. doi: 10.1358/dnp.2001.14.7.660941. PMID: 12813582. 17: Cohen JE, Onyike CU, McElroy VL, Lin AH, Abrams TW. Pharmacological characterization of an adenylyl cyclase-coupled 5-HT receptor in aplysia: comparison with mammalian 5-HT receptors. J Neurophysiol. 2003 Mar;89(3):1440-55. doi: 10.1152/jn.01004.2002. Epub 2002 Nov 20. PMID: 12611939. 18: Russell MG, Dias R. Memories are made of this (perhaps): a review of serotonin 5-HT(6) receptor ligands and their biological functions. Curr Top Med Chem. 2002 Jun;2(6):643-54. doi: 10.2174/1568026023393877. PMID: 12052198. 19: Meneses A. Tianeptine: 5-HT uptake sites and 5-HT(1-7) receptors modulate memory formation in an autoshaping Pavlovian/instrumental task. Neurosci Biobehav Rev. 2002 May;26(3):309-19. doi: 10.1016/s0149-7634(02)00005-2. PMID: 12034133. 20: Shirazi-Southall S, Rodriguez DE, Nomikos GG. 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. doi: 10.1016/S0893-133X(01)00400-6. PMID: 11927183.