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RS 42358-197

Catalog No. T20739 CAS 135729-55-4

Synonyms: RS-42358-197, RS42358-197, RS 25259-007

RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist.

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RS 42358-197, CAS 135729-55-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 282.00
2 mg	In stock	$ 423.00
5 mg	In stock	$ 651.00
10 mg	In stock	$ 976.00
25 mg	In stock	$ 1,450.00
50 mg	In stock	$ 1,960.00
100 mg	In stock	$ 2,630.00
1 mL * 10 mM (in DMSO)	In stock	$ 646.00

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Purity: 98.23%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	RS 42358-197 (RS 25259-007) is a competitive 5-HT3 receptor antagonist.
In vitro	RS 42358-197 acts against 5-HT-induced contractions in the guinea pig ileum (low-potency phase), yielding a pA2 estimate of 8.1[1].
In vivo	In anesthetized rats. RS 42358-197, administered by the intravenous, intraduodenal or transdermal route, dose-dependently inhibited the Bezold-Jarisch reflex induced by 2-methyl 5-HT (ID50:0.05 micrograms/kg; i.v., 5.7 micrograms/kg; i.d., and 11.6 micrograms/chamber, respectively). In this regard, when administered intraduodenally, RS 42358-197 was more potent and exhibited a longer duration of action than either ondansetron or granisetron. In dogs, RS 42358-197, administered either intravenously or orally, dose-dependently inhibited the emesis induced by cisplatin, actinomycin and cyclophosphamide, but not that induced by apomorphine. When tested at maximally effective doses against cisplatin-induced emesis in dogs, RS 42358-197 had a longer duration of antiemetic activity (> 6 h) than ondansetron (2 h). RS 42358-197, administered orally, also afforded protection against cisplatin-induced emesis in ferrets. At doses that showed marked anti-emetic activity in dogs (10-100 micrograms/kg; i.v. and 100-1000 micrograms/kg; i.d.), RS 42358-197 did not produce any hemodynamic changes[1].

Synonyms	RS-42358-197, RS42358-197, RS 25259-007
Molecular Weight	330.85
Formula	C19H23ClN2O
CAS No.	135729-55-4

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11 mg/mL (33.25 mM)

References and Literature

1. Costall B, et al. The effect of the 5-HT3 receptor antagonist, RS-42358-197, in animal models of anxiety. Eur J Pharmacol. 1993 Mar 30;234(1):91-9. 2. Eglen RM, et al. RS 42358-197, a novel and potent 5-HT3 receptor antagonist, in vitro and in vivo. J Pharmacol Exp Ther. 1993 Aug;266(2):535-43. 3. Wong EH, Bonhaus DW, Wu I, Stefanich E, Eglen RM. Labelling of 5-hydroxytryptamine3 receptors with a novel 5-HT3 receptor ligand, [3H]RS-42358-197. J Neurochem. 1993 Mar;60(3):921-30. 4. Bonhaus DW, et al. Pharmacological characterization of 5-hydroxytryptamine3 receptors in murine brain and ileum using the novel radioligand [3H]RS-42358-197: evidence for receptor heterogeneity. J Neurochem. 1993 Nov;61(5):1927-32.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library

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Keywords

RS 42358-197 135729-55-4 GPCR/G Protein Neuroscience 5-HT Receptor RS-42358-197 RS42358-197 RS 25259-007 inhibitor inhibit

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