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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, ...

Schoeffter, P. et al., Bell, R. et al., Fregoneze, J.B. et al., Millan, M.J. et al., Bell, R. et al., et al.

Héry, François-Bellan, Héry, Deprez, Becquet,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Psychiatry related information on Sdz 216-525

Effects of (-)-pindolol and SDZ 216-525 on social and agonistic behavior in mice [1].
In view of conflicting results reported for 5-HT1A receptor involvement in murine social conflict, this study examined the effect of two compounds, SDZ 216-525 and (-)-pindolol, on agonistic and social behavior in male mice [1].

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

Current results are consistent with data for the lack of effect of WAY-100635 on rat agonistic behavior but contrast with findings for the effects of the 5-HT1A receptor antagonists (+)-WAY-100135 and SDZ 216-525 on mouse agonistic behavior [7].

Biological context of Sdz 216-525

SDZ 216-525, a selective 5-HT1A receptor antagonist, reverts zinc-induced inhibition of water intake in dehydrated rats [8].

Anatomical context of Sdz 216-525

The novel 5-HT1A receptor antagonist, SDZ 216-525, decreases 5-HT release in rat hippocampus in vivo [9].
Third ventricle injections of SDZ 216-525, a selective 5-HT1A receptor antagonist, 45 min before zinc administration, generated a dose-dependent reversal of zinc-induced thirst blockade in water-deprived rats [8].

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].

References

Effects of (-)-pindolol and SDZ 216-525 on social and agonistic behavior in mice. Bell, R., Hobson, H. Pharmacol. Biochem. Behav. (1993) [Pubmed]
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]
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]
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]
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]
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]
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]
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]
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]
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]
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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