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Chemical Compound Review

CHEMBL22564     3-[4-(2- methoxyphenyl)piperazin-1- yl]-2...

Synonyms: SureCN2230435, CHEBI:128476, Way-100135, AC1L3GJK, WAY-100,135, ...
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Disease relevance of Way 100135

  • Both pindolol, a nonselective 5-HT1A receptor/beta adrenoceptor antagonist and n-t-butyl,-3-[1-[4-(2-methoxy)phenyl]piperazinyl]-1-phenylpropionamid e [(+) WAY 100135], a more selective 5-HT1A receptor antagonist, dose dependently attenuated the hypothermia induced by all three agonists [1].

Psychiatry related information on Way 100135

  • Given alone, WAY 100135 had no effect on the locomotor activity of rats; 2) WAY 100135 (1.25 and 2.5 mg/kg, but not 10 or 20 mg/kg), attenuated or abolished the disruptive effects of MK-801 on the sensorimotor gating measured in a prepulse-induced inhibition of the acoustic startle response paradigm [2].

High impact information on Way 100135

  • This inhibition was not affected by previous systemic application of either the selective 5HT1A receptor antagonist (+)WAY 100135 or by the 5HT2 receptor antagonist mesulergine, whereas pretreatment with the nonselective 5HT1 antagonist methiothepin significantly attenuated the effect of TFMPP [3].
  • The effect of 8-OH-DPAT was reversed by WAY 100135 [N-tert-butyl-3-[1-[1-(2-methoxy)phenyl]piperazinyl]-1-phenylpropiona mide; a 5-HT1A antagonist] [4].
  • The 5-HT(1A) receptor agonist buspirone relaxed fundic smooth muscle, and the relaxation was inhibited by WAY-100135 but not by N(omega)-nitro-l-arginine or tetrodotoxin [5].
  • These results indicate that WAY 100135 is a silent and selective 5-HT1A antagonist whereas SDZ 216-525 demonstrates a partial agonist activity at the somatodendritic 5-HT1A autoreceptor in the guinea-pig DRN [6].
  • The decrease in heart rate produced by i.v. bolus doses of flesinoxan or U-93385 was reversed by administration of the 5-HT1A receptor antagonists spiperone or WAY 100135 [7].

Biological context of Way 100135


Anatomical context of Way 100135


Associations of Way 100135 with other chemical compounds

  • The effects of a low dose of 5-HT (3.2 microM) on fPS, Vr and R in were reversed by the specific 5-HT(1A)-receptor antagonist WAY 100135 (10 microM). cOA (1 microM) failed to potentiate 5-HT1A receptor mediated effects on fPS, Vr or R in [12].
  • Antidepressant properties of 5-HT1A receptor ligands (the full agonist 8-OH-DPAT, the partial agonists ipsapirone and buspirone, and the selective antagonist WAY 100135) were studied in a chronic mild stress model of depression [13].
  • As 5-hydroxytryptamine1A (5-HT1A) receptors are enriched on cell bodies of corticostriatal neurones, a selective 5-HT1A-antagonist (WAY 100135) was coapplied with the lower dose of NMDA [14].
  • The full 5-HT1A receptor agonist BAY R 1531 blocked, whereas, WAY 100135 and gepirone intensified 30-bites analgesia [11].
  • In order to assess whether these ligands decrease 5-HT release by stimulating 5-HT1A receptors we examined the ability of the selective 5-HT1A receptor antagonist N-tert-butyl 3-4-(2-methoxyphenyl) piperazin-1-yl-2-phenylpropanamide dihydrochloride (WAY-100135) to block their inhibitory effects on 5-HT [15].

Gene context of Way 100135


Analytical, diagnostic and therapeutic context of Way 100135


  1. 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]
  2. WAY 100135, an antagonist of 5-HT1A serotonin receptors, attenuates psychotomimetic effects of MK-801. Wedzony, K., Maćkowiak, M., Zajaczkowski, W., Fijał, K., Chocyk, A., Czyrak, A. Neuropsychopharmacology (2000) [Pubmed]
  3. 5HT1B receptor agonists inhibit light-induced phase shifts of behavioral circadian rhythms and expression of the immediate-early gene c-fos in the suprachiasmatic nucleus. Pickard, G.E., Weber, E.T., Scott, P.A., Riberdy, A.F., Rea, M.A. J. Neurosci. (1996) [Pubmed]
  4. The effects of serotonin on glucocorticoid receptor binding in rat raphe nuclei and hippocampal cells in culture. Héry, M., Sémont, A., Fache, M.P., Faudon, M., Héry, F. J. Neurochem. (2000) [Pubmed]
  5. Serotonergic modulation of murine fundic tone. Xue, L., Camilleri, M., Locke, G.R., Schuurkes, J.A., Meulemans, A., Coulie, B.J., Szurszewski, J.H., Farrugia, G. Am. J. Physiol. Gastrointest. Liver Physiol. (2006) [Pubmed]
  6. Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus. Mundey, M.K., Fletcher, A., Marsden, C.A. Neuropharmacology (1994) [Pubmed]
  7. Tolerance development to the vagal-mediated bradycardia produced by 5-HT1A receptor agonists. McCall, R.B., Escandon, N.A., Harris, L.T., Clement, M.E. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  8. Evidence for the involvement of the 5-HT1A receptor in CCK induced satiety in rats. Voigt, J.P., Fink, H., Marsden, C.A. Naunyn Schmiedebergs Arch. Pharmacol. (1995) [Pubmed]
  9. Structure-activity relationship studies of CNS agents. Part 24: New analogs of N-tert.-butyl-3-[4-(2-methoxyphenyl)-1-piperazinyl]-2-phenylpropanamide (WAY-100135). Boksa, J., Klodzińska, A., Charakchieva-Minol, S., Chojnacka-Wójcik, E., Mokrosz, J.L. Die Pharmazie. (1996) [Pubmed]
  10. The antagonist actions of WAY-100135 and its enantiomers on 5-HT1A receptor-mediated hyperpolarization of the rat isolated superior cervical ganglion. Rhodes, K.F., Dover, G., Lattimer, N. Naunyn Schmiedebergs Arch. Pharmacol. (1993) [Pubmed]
  11. Involvement of the midbrain periaqueductal gray 5-HT1A receptors in social conflict induced analgesia in mice. Canto-de-Souza, A., Nunes de Souza, R.L., Pelá, I.R., Graeff, F.G. Eur. J. Pharmacol. (1998) [Pubmed]
  12. The sleep inducing brain lipid cis-oleamide (cOA) does not modulate serotonergic transmission in the CA1 pyramidal neurons of the hippocampus in vitro. Dougalis, A., Lees, G., Ganellin, C.R. Neuropharmacology (2004) [Pubmed]
  13. The effect of 5-HT1A receptor ligands in a chronic mild stress model of depression. Przegaliński, E., Moryl, E., Papp, M. Neuropharmacology (1995) [Pubmed]
  14. NMDA-induced glutamate and aspartate release from rat cortical pyramidal neurones: evidence for modulation by a 5-HT1A antagonist. Dijk, S.N., Francis, P.T., Stratmann, G.C., Bowen, D.M. Br. J. Pharmacol. (1995) [Pubmed]
  15. Differential effects of WAY-100135 on the decrease in 5-hydroxytryptamine release induced by buspirone and NAN-190. Routledge, C., Gurling, J., Ashworth-Preece, M.A., Dourish, C.T. Eur. J. Pharmacol. (1995) [Pubmed]
  16. Role of 5-HT in stress, anxiety, and depression. Graeff, F.G., Guimarães, F.S., De Andrade, T.G., Deakin, J.F. Pharmacol. Biochem. Behav. (1996) [Pubmed]
  17. Correlation between 5-HT7 receptor affinity and protection against sound-induced seizures in DBA/2J mice. Bourson, A., Kapps, V., Zwingelstein, C., Rudler, A., Boess, F.G., Sleight, A.J. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
  18. Role of hippocampal 5-HT1A receptors on elevated plus maze exploration after a single restraint experience. Netto, S.M., Guimarães, F.S. Behav. Brain Res. (1996) [Pubmed]
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