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Chemical Compound Review

Alnespiron     8-[4-[(5-methoxychroman-3- yl)-propyl...

Synonyms: AC1L3TIP, LS-173177, LS-173178, S-20244, S-20499, ...
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Psychiatry related information on 8-[4-[(5-methoxychroman-3-yl)-propyl-amino]butyl]-8-azaspiro[4.5]decane-7,9-dione

 

High impact information on 8-[4-[(5-methoxychroman-3-yl)-propyl-amino]butyl]-8-azaspiro[4.5]decane-7,9-dione

  • Autoradiographic analysis revealed a significant reduction of [3H]8-OH-DPAT and [3H]WAY-100635 (3H-labeled N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridyl)cyclohexa necarboxamide x 3HCl¿ binding to somatodendritic 5-HT1A receptors (but not to postsynaptic 5-HT1A receptors) of rats pretreated with alnespirone but not with 8-OH-DPAT [1].
  • The treatment with alnespirone did not modify baseline 5-HText but significantly attenuated the ability of 0.3 mg/kg s.c. alnespirone to reduce 5-HText in the dorsal raphe nucleus (DRN) and frontal cortex [1].
  • Differential regulation of somatodendritic serotonin 5-HT1A receptors by 2-week treatments with the selective agonists alnespirone (S-20499) and 8-hydroxy-2-(Di-n-propylamino)tetralin: microdialysis and autoradiographic studies in rat brain [1].
  • Anticonflict and discriminative stimulus effects in the pigeon of a new methoxy-chroman 5-HT1A agonist, (+)S 20244 and its enantiomers (+)S 20499 and (-)S 20500 [5].
  • The effects of three chemically dissimilar 5-HT1A agonists administered s.c. [8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), gepirone, and (+)4-[n-5-(methoxychroman-3-yl)n-propylamino]butyl-8-azaspiro++ +[4,5] decane-7,adione ((+) S-20499)] on both of these responses were studied [6].
 

Biological context of 8-[4-[(5-methoxychroman-3-yl)-propyl-amino]butyl]-8-azaspiro[4.5]decane-7,9-dione

 

Anatomical context of 8-[4-[(5-methoxychroman-3-yl)-propyl-amino]butyl]-8-azaspiro[4.5]decane-7,9-dione

  • In vitro binding assays revealed that these drugs bound with high affinity to 5-HT1A sites in hippocampal membranes (Ki: 0.19 nM for (+)-S 20499, 0.95 nM for (-)-S 20500 and 0.35 nM for the racemate (+/-) S 20244) [10].
  • In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity [11].
  • Subjects treated with 0.5 mg/kg of 8-OH-DPAT and 10 mg/kg of (+) S-20499 displayed in the initial time period "ballistic-type" rapid forelimb movements targeted toward the side of the head [12].
 

Associations of 8-[4-[(5-methoxychroman-3-yl)-propyl-amino]butyl]-8-azaspiro[4.5]decane-7,9-dione with other chemical compounds

 

Gene context of 8-[4-[(5-methoxychroman-3-yl)-propyl-amino]butyl]-8-azaspiro[4.5]decane-7,9-dione

References

  1. Differential regulation of somatodendritic serotonin 5-HT1A receptors by 2-week treatments with the selective agonists alnespirone (S-20499) and 8-hydroxy-2-(Di-n-propylamino)tetralin: microdialysis and autoradiographic studies in rat brain. Casanovas, J.M., Vilaró, M.T., Mengod, G., Artigas, F. J. Neurochem. (1999) [Pubmed]
  2. Selective antiaggressive effects of alnespirone in resident-intruder test are mediated via 5-hydroxytryptamine1A receptors: A comparative pharmacological study with 8-hydroxy-2-dipropylaminotetralin, ipsapirone, buspirone, eltoprazine, and WAY-100635. de Boer, S.F., Lesourd, M., Mocaer, E., Koolhaas, J.M. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  3. Antidepressant-like effects of alnespirone (S 20499) in the learned helplessness test in rats. Mac Sweeney, C.P., Lesourd, M., Gandon, J.M. Eur. J. Pharmacol. (1998) [Pubmed]
  4. Alnespirone and buspirone have anxiolytic-like effects in a conflict procedure in rats by stimulating 5-HT(1A) receptors. Cervo, L., Munoz, C., Bertaglia, A., Samanin, R. Behavioural pharmacology. (2000) [Pubmed]
  5. Anticonflict and discriminative stimulus effects in the pigeon of a new methoxy-chroman 5-HT1A agonist, (+)S 20244 and its enantiomers (+)S 20499 and (-)S 20500. Barrett, J.E., Gamble, E.H., Zhang, L., Guardiola-Lemaitre, B. Psychopharmacology (Berl.) (1994) [Pubmed]
  6. Differential induction of 5-HT1A-mediated responses in vivo by three chemically dissimilar 5-HT1A agonists. Scott, P.A., Chou, J.M., Tang, H., Frazer, A. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  7. 5-HT1A receptor agonists prevent in rats the yawning and penile erections induced by direct dopamine agonists. Simon, P., Guardiola, B., Bizot-Espiard, J., Schiavi, P., Costentin, J. Psychopharmacology (Berl.) (1992) [Pubmed]
  8. Production and characterization of polyclonal anti-S 20499 antibodies: influence of the hapten structure on stereospecificity. Got, P.A., Guillaumet, G., Boursier-Neyret, C., Scherrmann, J.M. Journal of pharmaceutical sciences. (1997) [Pubmed]
  9. Neuroendocrine profile of the potential anxiolytic drug S-20499. Levy, A.D., Li, Q., Gustafson, M., Van de Kar, L.D. Eur. J. Pharmacol. (1995) [Pubmed]
  10. New methoxy-chroman derivatives, 4[N-(5-methoxy-chroman-3-yl)N- propylamino]butyl-8-azaspiro-(4,5)-decane-7,9-dione [(+/-)-S 20244] and its enantiomers, (+)-S 20499 and (-)-S 20500, with potent agonist properties at central 5-hydroxytryptamine1A receptors. Kidd, E.J., Haj-Dahmane, S., Jolas, T., Lanfumey, L., Fattaccini, C.M., Guardiola-Lemaitre, B., Gozlan, H., Hamon, M. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  11. In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity. Astier, B., Lambás Señas, L., Soulière, F., Schmitt, P., Urbain, N., Rentero, N., Bert, L., Denoroy, L., Renaud, B., Lesourd, M., Muñoz, C., Chouvet, G. Eur. J. Pharmacol. (2003) [Pubmed]
  12. An ethopharmacological analysis of selective activation of 5-HT1A receptors: the mouse 5-HT1A syndrome. Blanchard, R.J., Griebel, G., Guardiola-Lemaître, B., Brush, M.M., Lee, J., Blanchard, D.C. Pharmacol. Biochem. Behav. (1997) [Pubmed]
  13. Activation of serotonergic neurotransmission during the performance of aggressive behavior in rats. van der Vegt, B.J., Lieuwes, N., van de Wall, E.H., Kato, K., Moya-Albiol, L., Martínez-Sanchis, S., de Boer, S.F., Koolhaas, J.M. Behav. Neurosci. (2003) [Pubmed]
  14. Similar pharmacological properties of 8-OH-DPAT and alnespirone (S 20499) at dopamine receptors: comparison with buspirone. Protais, P., Lesourd, M., Comoy, E. Eur. J. Pharmacol. (1998) [Pubmed]
  15. A comparison of the oxytocin and vasopressin responses to the 5-HT1A agonist and potential anxiolytic drug alnespirone (S-20499). Van de Kar, L.D., Levy, A.D., Li, Q., Brownfield, M.S. Pharmacol. Biochem. Behav. (1998) [Pubmed]
 
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