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Chemical Compound Review

SPIROXAMIDE     8-(7,10- dioxabicyclo[4.4.0]deca- 1,3,5...

Synonyms: Spiroxatrine, Espiroxatrina, Spiroxatrinum, AGN-PC-000HKU, CHEMBL300555, ...
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Disease relevance of Spiroxatrine


Psychiatry related information on Spiroxatrine


High impact information on Spiroxatrine

  • Spiroxatrine was identified as a moderately potent (K:(i)=118 nM) but non-selective agonist at the human nociceptin/orphanin FQ receptor, ORL1 [5].
  • Moreover, the good affinity of [125I] rauwolscine-OHPC binding sites for spiroxatrine, yohimbine, WB 4101, the relatively good affinity for prazosin (Ki =37.4 nM) and the affinity ratio prazosin/oxymetazoline (37.4/43.4=0.86) were consistent with an alpha2C selective labelling of [125I]rauwolscine-OHPC [6].
  • In contrast to sigma ligands and other reference compounds, the 5-HT1A agonists buspirone, 8-OH-DPAT and spiroxatrine dose-dependently produced BMY 14802-like discriminative stimulus effects [7].
  • The inhibition was blocked by spiroxatrine indicating it was mediated by 5-HT1A receptors [8].
  • 3. The putative 5-HT1A antagonists, spiroxatrine (1-30 mg kg-1, p.o.), (+/-)-pindolol (30 mg kg-1, p.o.) and methiothepin (3-10 mg kg-1, p.o.), each attenuated the 8-OH-DPAT (3 mg kg-1, s.c.)-induced increase in mobility [9].

Biological context of Spiroxatrine


Anatomical context of Spiroxatrine


Associations of Spiroxatrine with other chemical compounds


Gene context of Spiroxatrine

  • In anaesthetized rats, the 5-HT1A antagonist, spiroxatrine (1 mg/kg), and the 5-HT3 receptor antagonist, MDL72222 (0.3 mg/kg), selectively diminished the hypotensive phase without affecting the pressor phase [20].
  • The 5-HT1A agonist 8-hydroxy-2-(di-N-propylamine)tetralin hydrobromide mimicked, whereas the 5-HT1A antagonist spiroxatrine blocked, these hyperpolarizing responses [21].
  • Whereas spiroxatrine (0.5 mg/kg s.c.) blocked the effect of buspirone on the colonic hypermotility induced by i.c.v. injection of CRF, BMY 14802 at a similar dose (0.5 mg/kg s.c.) was unable to block the action of buspirone [14].
  • Metitepine and methysergide antagonized the inhibitory effect of 5-HT, whereas spiroxatrine, propranolol, ketanserin and ICS 205-930 did not [22].
  • The administration of the 5HT1A agonist (8-hydroxy 2-n-dipropylamino tetralin) resulted in a significant increase in plasma prolactin and that of the specific 5HT1A antagonist spiroxatrine had the opposite effect [23].

Analytical, diagnostic and therapeutic context of Spiroxatrine

  • Seizure discharge activity was attenuated by the microinjection of the 5-HT1A agonist, 8-hydroxy-2-(di-N-propylamino)tetralin(8-(OH)-DPAT) and augmented by the specific 5-HT1A antagonist, spiroxatrine in the contralateral hippocampal CA-3 region [24].


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  2. 8OH-DPAT-Induced ocular hypotension: sites and mechanisms of action. Chu, T.C., Ogidigben, M.J., Potter, D.E. Exp. Eye Res. (1999) [Pubmed]
  3. Pharmacological analysis of the cardiac effects of 5-HT and some 5-HT receptor agonists in the pithed rat. Dabiré, H., Chaouche-Teyara, K., Cherqui, C., Fournier, B., Schmitt, H. Fundamental & clinical pharmacology. (1992) [Pubmed]
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  5. (8-Naphthalen-1-ylmethyl-4-oxo-1-phenyl-1,3,8-triaza-spiro[4. 5]dec-3-yl)-acetic acid methyl ester (NNC 63-0532) is a novel potent nociceptin receptor agonist. Thomsen, C., Hohlweg, R. Br. J. Pharmacol. (2000) [Pubmed]
  6. Characterization of a new radioiodinated probe for the alpha2C adrenoceptor in the mouse brain. Dossin, O., Moulédous, L., Baudry, X., Tafani, J.A., Mazarguil, H., Zajac, J.M. Neurochem. Int. (2000) [Pubmed]
  7. Discriminative stimulus characteristics of BMY 14802 in the pigeon. Vanecek, S.A., Essman, W.D., Taylor, D.P., Woods, J.H. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  8. 5-HT1A and 5-HT4 receptor colocalization on hippocampal pyramidal cells. Roychowdhury, S., Haas, H., Anderson, E.G. Neuropharmacology (1994) [Pubmed]
  9. Mediation of the antidepressant-like effect of 8-OH-DPAT in mice by postsynaptic 5-HT1A receptors. Luscombe, G.P., Martin, K.F., Hutchins, L.J., Gosden, J., Heal, D.J. Br. J. Pharmacol. (1993) [Pubmed]
  10. 5-HT1A-agonistic properties of naftopidil, a novel antihypertensive drug. Borbe, H.O., Metzenauer, P., Szelenyi, I. Eur. J. Pharmacol. (1991) [Pubmed]
  11. Vasodilatation elicited by 5-HT1A receptor agonists in constant-pressure-perfused rat kidney is mediated by blockade of alpha 1A-adrenoceptors. Eltze, M., Boer, R., Sanders, K.H., Kolassa, N. Eur. J. Pharmacol. (1991) [Pubmed]
  12. Involvement of brain 5-HT1A receptors in the hypotensive response to urapidil. Kolassa, N., Beller, K.D., Sanders, K.H. Am. J. Cardiol. (1989) [Pubmed]
  13. Stimulation of hippocampal 5-HT1A receptors causes amnesia and anxiolytic-like but not antidepressant-like effects in the rat. Carli, M., Tatarczynska, E., Cervo, L., Samanin, R. Eur. J. Pharmacol. (1993) [Pubmed]
  14. Buspirone inhibits corticotropin-releasing factor and stress-induced cecal motor response in rats by acting through 5-HT1A receptors. Martinez, J.A., Buéno, L. Eur. J. Pharmacol. (1991) [Pubmed]
  15. Behavioral and neurochemical effects of the serotonin (5-HT)1A receptor ligand spiroxatrine. Barrett, J.E., Hoffmann, S.M., Olmstead, S.N., Foust, M.J., Harrod, C., Weissman, B.A. Psychopharmacology (Berl.) (1989) [Pubmed]
  16. 5-hydroxytryptamine (5-HT)1A receptors and the tail-flick response. I. 8-hydroxy-2-(di-n-propylamino) tetralin HBr-induced spontaneous tail-flicks in the rat as an in vivo model of 5-HT1A receptor-mediated activity. Millan, M.J., Bervoets, K., Colpaert, F.C. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  17. [3H]dihydroergotamine as a high-affinity, slowly dissociating radioligand for 5-HT1B binding sites in rat brain membranes: evidence for guanine nucleotide regulation of agonist affinity states. Hamblin, M.W., Ariani, K., Adriaenssens, P.I., Ciaranello, R.D. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  18. Antagonism of 8-OH-DPAT-induced behaviour in rats. Berendsen, H.H., Broekkamp, C.L., Van Delft, A.M. Eur. J. Pharmacol. (1990) [Pubmed]
  19. Characterization of DOI, a putative 5-HT2 receptor agonist in the rat. Dabiré, H., Chaouche-Teyara, K., Cherqui, C., Fournier, B., Laubie, M., Schmitt, H. Eur. J. Pharmacol. (1989) [Pubmed]
  20. Characterization of the biphasic blood pressure response to alpha-methyl-5-hydroxytryptamine in anaesthetized rats. Balasubramaniam, G., Lee, H.S., Mah, S.C. Archives internationales de pharmacodynamie et de thérapie. (1995) [Pubmed]
  21. Diverse actions of 5-hydroxytryptamine on frog spinal dorsal horn neurons in vitro. Tan, H., Miletic, V. Neuroscience (1992) [Pubmed]
  22. Inhibition of noradrenaline release from the sympathetic nerves of the human saphenous vein via presynaptic 5-HT receptors similar to the 5-HT 1D subtype. Molderings, G.J., Werner, K., Likungu, J., Göthert, M. Naunyn Schmiedebergs Arch. Pharmacol. (1990) [Pubmed]
  23. Effects of serotonergic agents on plasma prolactin levels in pyridoxine-deficient adult male rats. Sharma, S.K., Dakshinamurti, K. Neurochem. Res. (1994) [Pubmed]
  24. Suppression of domoic acid induced seizures by 8-(OH)-DPAT. Sharma, S.K., Dakshinamurti, K. J. Neural Transm. Gen. Sect. (1993) [Pubmed]
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