57477-39-1 Usage
Uses
BRL-53443 is a potent 5-HT and dopamine receptor agonist. Neuroresearch product.
Biological Activity
A potent 5-ht 1E/1F receptor agonist (pEC 50 values are 8.5 and 8.6 respectively). Displays > 30-fold selectivity over other 5-HT and dopamine receptors (pK i values are 8.7. 8.9, 7.2, 6.9, 7.2, 5.9, 7.0, 6.5, < 6, < 6, 6.3 and 6.2 for human 5-HT 1E , 1F , 1A , 1B , 1D , 2A , 2B , 2C , 4 , 7 , D 2 and D 3 receptors respectively). Induces 5-HT 2A receptor-mediated mouse aortic contraction in vitro (pEC 50 = 6.52). Active in vivo .
references
1. a.m. brown, k. avenell, t j. young et al. brl 54443, a potent agonist with selectivity for human cloned 5-ht1e and 5-ht1f receptors. 1998. br.j.pharmacol. 123 233p.2. s. lightowler, t. stean, n. upton et al. effect of brl 54443 (3-(1-methylpiperidin-4-yl)-1h-indol-5-ol), a 5-ht1e/1f receptor agonist, on general behaviour and maximal electroshock seizure threshold in the rat. 1998. br.j.pharmacol. 123 237p.3. mckune cm, watts sw. characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. j pharmacol exp ther. 2001 apr;297(1):88-95.4. janssen p, tack j, sifrim d et al. influence of 5-ht1 receptor agonists on feline stomach relaxation. eur j pharmacol. 2004 may 25;492(2-3):259-67.
Check Digit Verification of cas no
The CAS Registry Mumber 57477-39-1 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,7,4,7 and 7 respectively; the second part has 2 digits, 3 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 57477-39:
(7*5)+(6*7)+(5*4)+(4*7)+(3*7)+(2*3)+(1*9)=161
161 % 10 = 1
So 57477-39-1 is a valid CAS Registry Number.
57477-39-1Relevant articles and documents
5-HT1F agonists
-
, (2008/06/13)
The present invention relates to a compound of formula (I): or a pharmaceutical acid addition salt thereof; which is useful for activating 5-HT1freceptors and inhibiting protein extravasation in a mammal.
Synthesis and Structure-Activity Relationships of 5-Substituted Tryptamine Derivatives of o-Tolylpiperazine as Agonists at 5-HT1D Receptors
Perez, M.,Pauwels, P. J.,Palmier, C.,John, G. W.,Valentin, J. P.,Halazy, S.
, p. 680 - 689 (2007/10/03)
Analogs of 1-[2-[3-(2-amino-ethyl)-1H-indol-5-yloxy]-acetyl]-4-[o-tolyl]-piperazide 1, recently reported as a novel potent 5HT1D agonist, have been prepared and tested as 5HT1A, 5HD1Dα and 5HT1Dβ ligands and eva