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Chemical Compound Review

SureCN1041165     methyl4-[4-[4-(7,9,9-trioxo- 9$l^{6}-thia...

Synonyms: SDZ-216525, Sdz-216-525, PDSP1_000565, PDSP2_000563, SDZ 216,525, ...
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Psychiatry related information on Sdz 216-525


High impact information on Sdz 216-525

  • A lack of specificity of NAN-190 (and possibly SDZ 216-525) at high doses may explain the failure of previous studies to detect a 5-HT1A receptor agonist action [2].
  • Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus [3].
  • These values compared favorably with those of the structurally related eltoprazine (8.0) and the proposed 5-HT1A antagonists NAN-190 (9.2), MDL 73005 EF (8.9), SDZ 216-525 (8.8), BMY 7378 (8.7), (-)-tertatolol (8.1), (-)-alprenolol (7.7), WAY 100,135 (7.5) and spiperone (6.9) [4].
  • In addition, the effects of 8-OH-DPAT were blocked by a 5-HT1A antagonist, SDZ 216-525 [5].
  • In radioligand binding studies, SDZ 216-525 showed high affinity and selectivity for 5-HT1A sites (pKD = 9.2) as compared to 5-HT1B, 5-HT1C, 5-HT1D, 5-HT2 and 5-HT3 sites (pKD = 6.0, 7.2, 7.5, 5.2 and 5.4, respectively) [6].

Chemical compound and disease context of Sdz 216-525


Biological context of Sdz 216-525


Anatomical context of Sdz 216-525


Associations of Sdz 216-525 with other chemical compounds

  • The pharmacological properties of SDZ 216-525, methyl 4-(4-[4-(1,1,3-trioxo-2H-1,2-benzoisothiazol-2-yl)butyl]-1-p iperazinyl)1H- indole-2-carboxylate, a new selective and potent 5-HT1A receptor antagonist, are described in vitro (and comparisons made with those of MDL 73005 and NAN 190, two putative 5-HT1A receptor antagonists) and in vivo [6].
  • This effect was blocked by ritanserin, a 5-HT2/7 receptor antagonist, but not by SDZ-216-525, a 5-HT1A antagonist [10].

Gene context of Sdz 216-525

  • The novel 5-HT1A antagonists, WAY 100,135, MDL 73005 EF and (very potently) SDZ 216-525 all blocked DIH [11].
  • SDZ 216-525 (0.025-1.0 mg/kg), a selective 5-HT1A antagonist, significantly attenuated offensive posturing and bite-attacks at 1.0 mg/kg, and all offensive behaviors nonsignificantly at the smaller doses tested [1].


  1. Effects of (-)-pindolol and SDZ 216-525 on social and agonistic behavior in mice. Bell, R., Hobson, H. Pharmacol. Biochem. Behav. (1993) [Pubmed]
  2. The role of 5-HT1A autoreceptors and alpha 1-adrenoceptors in the inhibition of 5-HT release--II NAN-190 and SDZ 216-525. Sharp, T., Umbers, V., Hjorth, S. Neuropharmacology (1996) [Pubmed]
  3. 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]
  4. Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists. Millan, M.J., Canton, H., Gobert, A., Lejeune, F., Rivet, J.M., Bervoets, K., Brocco, M., Widdowson, P., Mennini, T., Audinot, V. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  5. Effects of serotonergic agonists on firing rates of photically responsive cells in the hamster suprachiasmatic nucleus. Ying, S.W., Rusak, B. Brain Res. (1994) [Pubmed]
  6. SDZ 216-525, a selective and potent 5-HT1A receptor antagonist. Schoeffter, P., Fozard, J.R., Stoll, A., Siegl, H., Seiler, M.P., Hoyer, D. Eur. J. Pharmacol. (1993) [Pubmed]
  7. Lack of effect of the 5-HT(1A) receptor antagonist WAY-100635 on murine agonistic behaviour. Bell, R., Lynch, K., Mitchell, P. Pharmacol. Biochem. Behav. (1999) [Pubmed]
  8. SDZ 216-525, a selective 5-HT1A receptor antagonist, reverts zinc-induced inhibition of water intake in dehydrated rats. Fregoneze, J.B., Ferreira, H., Soares, T., Luz, C.P., Bulcão, C., Nascimento, T., Marinho, C.A., Sarmento, C., De-Oliveira, I.R., Cunha, M. Braz. J. Med. Biol. Res. (1995) [Pubmed]
  9. The novel 5-HT1A receptor antagonist, SDZ 216-525, decreases 5-HT release in rat hippocampus in vivo. Sharp, T., McQuade, R., Fozard, J.R., Hoyer, D. Br. J. Pharmacol. (1993) [Pubmed]
  10. Serotonin directly stimulates luteinizing hormone-releasing hormone release from GT1 cells via 5-HT7 receptors. Héry, M., François-Bellan, A.M., Héry, F., Deprez, P., Becquet, D. Endocrine (1997) [Pubmed]
  11. Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists. Millan, M.J., Rivet, J.M., Canton, H., Le Marouille-Girardon, S., Gobert, A. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
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