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Chemical Compound Review

CHEMBL28000     N-[2-[4-(7-methoxynaphthalen- 1...

Synonyms: SureCN7116023, S-14671, AC1L300T, L001251, S 14671, ...
 
 
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Disease relevance of S-14671

  • In vivo, S 14671 induced the typical 5-HT1A agonist-induced responses of hypothermia and spontaneous tail-flicks at doses as low as greater than or equal to 5 micrograms/kg s.c. and greater than or equal to 40 micrograms/kg s.c., respectively [1].
 

High impact information on S-14671

  • S 14671 showed a very high affinity for 5-HT1A sites (pKi, 9.3) as compared to the reference ligands (pKi values, 9.2, 8.7, 8.7, 7.9 and 8.7, respectively) [2].
  • Furthermore, S 14671 acted as an antagonist of 5-HT-stimulated phosphoinositide turnover in rat choroid plexus (5-HT1C) and cortex (5-HT2) [2].
  • Although showing low affinity at 5-HT1B and 5-HT3 sites, S 14671 displayed significant affinity at both 5-HT1C and 5-HT2 sites; pKi, 7.8 in each case [2].
  • Activation of presynaptic receptors was demonstrated by inhibition of the electrical activity of the dorsal raphe nucleus with the following order of relative potency: S 14671 greater than 8-OH-DPAT greater than WY 50,324 greater than BMY 7378 greater than buspirone [2].
  • Spiperone, which acts as a pure 5-HT1A antagonist at raphe 5-HT1A receptors, blocked the action of S 14671 [2].
 

Anatomical context of S-14671

  • Buspirone, 8-OH-DPAT and S 14671 (1-[2-(2-thenoylamino)ethyl]- 4[1-(7-methoxynaphtyl)]-piperazine), claimed to be 5-HT1A receptor agonists, did not reduce forskolin-stimulated cAMP formation in the cerebral cortex [3].
 

Associations of S-14671 with other chemical compounds

  • In vivo, they both dose dependently blocked the flat-body posture and corticosterone secretion provoked by an action of the 5-HT1A receptor agonist, S 14671 (1-[2-(2-thenoyl-amino)ethyl]-4-[1-(7- methoxynaphtyl)]piperazine), at postsynaptic 5-HT1A receptors [4].
  • The anticonflict activity of S 14671 (0.01 mg/kg) was significantly antagonised by the 5-HT1A receptor antagonist, (-)-alprenolol (10 mg/kg), but not by combined treatment with the selective beta 1 receptor antagonist, betaxolol, and the selective beta 2 receptor antagonist, ICI 118,551 [5].

References

  1. S 14671: a novel naphthylpiperazine 5-HT1A agonist of high efficacy and exceptional in vivo potency. Millan, M.J., Canton, H., Rivet, J.M., Lejeune, F., Laubie, M., Lavielle, G. Eur. J. Pharmacol. (1991) [Pubmed]
  2. S 14671: a naphtylpiperazine 5-hydroxytryptamine1A agonist of exceptional potency and high efficacy possessing antagonist activity at 5-hydroxytryptamine1C/2 receptors. Millan, M.J., Rivet, J.M., Canton, H., Lejeune, F., Bervoets, K., Brocco, M., Gobert, A., Lefebvre de Ladonchamps, B., Le Marouille-Girardon, S., Verriele, L. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  3. BIMT 17, a 5-HT2A receptor antagonist and 5-HT1A receptor full agonist in rat cerebral cortex. Borsini, F., Giraldo, E., Monferini, E., Antonini, G., Parenti, M., Bietti, G., Donetti, A. Naunyn Schmiedebergs Arch. Pharmacol. (1995) [Pubmed]
  4. WAY 100,135 and (-)-tertatolol act as antagonists at both 5-HT1A autoreceptors and postsynaptic 5-HT1A receptors in vivo. Lejeune, F., Rivet, J.M., Gobert, A., Canton, H., Millan, M.J. Eur. J. Pharmacol. (1993) [Pubmed]
  5. Involvement of 5-HT1A receptors in the anxiolytic action of S 14671 in the pigeon conflict test. Schreiber, R., Brocco, M., de Ladonchamps, B.L., Millan, M.J. Pharmacol. Biochem. Behav. (1995) [Pubmed]
 
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