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Chemical Compound Review

AC1MTQU1     3-[4-(3- chlorophenyl)piperazin-1-yl]- 1,1...

Synonyms: CHEMBL534232, SureCN7741355, CHEBI:64060, BRL-15572, CCG-204280, ...
 
 
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High impact information on BRL15572

  • Interestingly, 5-CT-induced cardiac sympatho-inhibition was abolished by methiothepin, the cocktail of antagonists/inhibitors, GR 127935 or the combination of SB224289 (5-HT1B) plus BRL15572 (5-HT1D), but remained unchanged when SB224289 or BRL15572 were given separately [1].
  • In contrast, BRL15572 had little or no effect on sumatriptan-induced contractions in the four blood vessels investigated [2].
  • The selective antagonist for the 5-HT(1B) receptors SB224289 dose-dependently blocked the effects of sumatriptan on large coronary and internal carotid arteries whereas the selective antagonist for the 5-HT(1D) receptors BRL15572 did not affect any of these effects [3].
  • On the other hand, 3-[4-(4-chlorophenyl)piperazin-1-yl]-1,1-diphenyl-2-propanol HCl (BRL15572), a selective antagonist against human 5-HT1D receptors, was inactive as an antagonist at least up to 1 microM [4].

References

  1. Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: correlation with 5-HT1 and putative 5-ht5A/5B receptors. Sánchez-Lopez, A., Centurión, D., Vázquez, E., Arulmani, U., Saxena, P.R., Villalón, C.M. Br. J. Pharmacol. (2003) [Pubmed]
  2. Characterization of sumatriptan-induced contractions in human isolated blood vessels using selective 5-HT(1B) and 5-HT(1D) receptor antagonists and in situ hybridization. van den Broek, R.W., Bhalla, P., VanDenBrink, A.M., de Vries, R., Sharma, H.S., Saxena, P.R. Cephalalgia : an international journal of headache. (2002) [Pubmed]
  3. Comparative effects of frovatriptan and sumatriptan on coronary and internal carotid vascular haemodynamics in conscious dogs. Carel, I., Ghaleh, B., Edouard, A., Dubois-Rande, J.L., Parsons, A.A., Giudicelli, J.F., Berdeaux, A. Br. J. Pharmacol. (2001) [Pubmed]
  4. 5-HT-stimulated [35S]guanosine-5'-O-(3-thio)triphosphate binding as an assay for functional activation of G proteins coupled with 5-HT1B receptors in rat striatal membranes. Odagaki, Y., Toyoshima, R. Naunyn Schmiedebergs Arch. Pharmacol. (2006) [Pubmed]
 
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