RS-127445 Inhibitor CAS No. 199864-87-3

Cat. No.	Name	Size	Price
KI1441	RS-127445	5 mg	$112
	RS-127445	10 mg	$176
	RS-127445	50 mg	$752

Chemical Characteristic

Product Name	RS-127445
CAS No.	199864-87-3
Molecular Weight	281.3
Formula	C₁₇H₁₆FN₃
Chemical Name	4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE;RS 127445 HYDROCHLORIDE
Smiles	c1(nc(cc(n1)C(C)C)c1ccc(c2ccccc12)F)N
Chemical Structure

Biological activities

RS-127445 is a 5-HT_{2B receptor antagonist. RS-127445 has nanomolar affinities for the 5-HT_{2B, 5-HT_{2A, 5-HT_{2C and 5-HT_{1A receptors with pKi of 9.5, 6.3, 6.4 and 5.5, respectively. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonizes 5-HT-evoked increases in intracellular calcium with a pIC50 of 10.4. RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus and (+)α-methyl-5-HT-mediated relaxation of the rat jugular vein. RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates. ^[1] RS-127445 (0.1-10 mM) concentration-dependently reduces peristaltic frequency. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output in vivo. ^[2] Pretreatment with RS-127445 completely (0.5 and 0.1 mg/kg) blocks 3,4-methylenedioxy- methamphetamine (MDMA)-induced locomotion in WT mice. RS-127445 (0.5 and 0.1 mg/kg), potently and completely reverses the hyperactivity caused by a dose (10 mg/kg) of MDMA in mice. ^[3]}}}}}

Protocols

RS-127445 is dissolved in DMSO. ^[2]

References

[1] Bonhaus DW, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999, 127(5): 1075-1082. [2] Bassil AK, et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br J Pharmacol. 2009, 158(1): 252-258. [3] Doly S, et al. Serotonin 5-HT2B receptors are required for 3,4-methylenedioxy- methamphetamine-induced hyperlocomotion and 5-HT release in vivo and in vitro. J Neurosci. 2008, 28(11): 2933-2940.

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