BRL-54443 - CAS 57477-39-1
Catalog number:
57477-39-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C14H18N2O
Molecular Weight:
230.31
COA:
Inquire
Targets:
5-HT Receptor
Description:
BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
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Purity:
>98%
MSDS:
Inquire
1.Influence of 5-HT1 receptor agonists on feline stomach relaxation.
Janssen P1, Tack J, Sifrim D, Meulemans AL, Lefebvre RA. Eur J Pharmacol. 2004 May 25;492(2-3):259-67.
Sumatriptan is known for its stomach relaxing properties in both humans and cats, but the receptor involved has not been characterized. In a barostat study the intragastric volume was monitored in sedated cats at constant pressure. The maximum intragastric volume increase after subcutaneous or intravenous administration of saline or agonists was registered [mean (n=4-5)]. Sumatriptan (0.01-1 mg kg(-1)) induced a dose-dependent intragastric volume increase vs. saline (4-15 vs. 5 ml, respectively) that was sometimes accompanied by retching after 8-10 min. Pre-treatment with nitric oxide-synthase inhibitors and different 5-HT(1) receptor antagonists N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-cyclohexanecarboxamide(WAY-100635), 2-methyl-4-(5-methyl-[1,2,4]oxadiazol-3-yl)-biphenyl-4-carboxylic-acid[4-methoxy-3-(4-methyl-piperazin-1-yl)-phenyl]amide(GR-127935), N-acetyl-5-hydroxytryptophyl-5-hydroxytryptophan-amide(5-HTP-DP) and 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine-HCl(NAN-190) did not affect the sumatriptan-induced effect.
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Chemical Structure

CAS 57477-39-1 BRL-54443

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