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Chemical Compound Review

buspirone     8-[4-(4-pyrimidin-2- ylpiperazin-1...

Synonyms: Buspinol, Buspisal, Ansiced, Anxiron, Buspirona, ...
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Disease relevance of buspirone


Psychiatry related information on buspirone


High impact information on buspirone


Chemical compound and disease context of buspirone


Biological context of buspirone


Anatomical context of buspirone

  • CONCLUSION: The study shows that buspirone modulates the immune system and leads to changes in the CD4 and CD8 T-cell numbers, functional capacity, cell maturation and viral load [23].
  • Furthermore, preclinical studies have shown that buspirone does not possess anticonvulsant or muscle relaxant properties and does not interact significantly with central nervous system depressants [24].
  • Development of "flu-like' symptoms, so severe that two patients withdrew from the study and two patients ceased medication before time, was a clinical indication of modulation of the immune system by buspirone [23].
  • (R)-8-OH-DPAT, (S)-8-OH-DPAT, and buspirone stimulated [35S]GTPgammaS binding in hippocampus by 340%, 140%, and 78%, with EC50 values of 71, 51, and 132 nM [25].
  • This incorporation could be blocked when membranes were incubated with 1 microM of several agents that have high affinity for 5-HT1A sites [5-HT, 8-hydroxy-2-(di-n-propylamino)tetraline, TVX Q 7821, spiperone, buspirone, d-lysergic acid diethylamide, metergoline] [26].

Associations of buspirone with other chemical compounds

  • In man, buspirone hydrochloride at doses of 30, 60, and 90 mg orally significantly elevated plasma prolactin (PRL) and growth hormone (GH) concentrations [13].
  • Spontaneous 5-HT1A receptor activity was partially attenuated by 5-HT1A receptor partial agonists with anxiolytic activity (e.g. buspirone and flesinoxan) but was not altered by full agonists or antagonists [27].
  • Obsessive-compulsive disorder, fluoxetine, and buspirone [28].
  • Not only does the lack of effect of buspirone on the Amphetamine and Morphine-Benzedrine Group subscales indicate lack of a euphorigenic property, but the score on the Lysergic Acid Diethylamide subscale, especially in the 40-mg group, suggests a dysphorigenic property at high doses [21].
  • By contrast, buspirone is 16-fold weaker at dopamine (D2) receptors (IC50 = 380 nM), whereas TVX Q 7821 is 6-fold less potent at alpha-adrenergic1 sites (IC50 = 58 nM) [29].

Gene context of buspirone


Analytical, diagnostic and therapeutic context of buspirone

  • These issues are discussed herein, using the clinical trials of buspirone, a new, nonsedating antianxiety agent, as a model for the process of drug selection [32].
  • The single-blind study, conducted in 23 outpatients, consisted of 28 days of buspirone treatment followed by four days of placebo treatment [33].
  • Buspirone was not removed by hemodialysis [20].
  • A small, transient pupillary constriction was evident in the 20- and 40-mg buspirone groups, but it dissipated within two hours after dosing [21].
  • Buspirone did not alter the EEG or DSST performance but did increase self-ratings of sedation and feeling "spacey" and impaired memory function; these effects generally were quantitatively less than with triazolam [34].


  1. High-dose buspirone in case of tardive dyskinesia. Neppe, V.M. Lancet (1989) [Pubmed]
  2. Treatment of cerebellar ataxia with buspirone: a double-blind study. Trouillas, P., Xie, J., Adeleine, P. Lancet (1996) [Pubmed]
  3. Buspirone in treatment of premenstrual syndrome. Rickels, K., Freeman, E., Sondheimer, S. Lancet (1989) [Pubmed]
  4. Panic and hypertension associated with single dose of buspirone. Chignon, J.M., Lepine, J.P. Lancet (1989) [Pubmed]
  5. Buspirone for anxiety disorders in patients with severe lung disease. Craven, J., Sutherland, A. Lancet (1991) [Pubmed]
  6. Buspirone metabolite and panic attacks. Fuller, R.W. Lancet (1990) [Pubmed]
  7. Short-term buspirone treatment in disinhibition with dementia. Tiller, J.W., Dakis, J.A., Shaw, J.M. Lancet (1988) [Pubmed]
  8. Buspirone treatment of Tourette's syndrome. Dursun, S.M., Burke, J.G., Reveley, M.A. Lancet (1995) [Pubmed]
  9. Buspirone treatment of anxious alcoholics. A placebo-controlled trial. Kranzler, H.R., Burleson, J.A., Del Boca, F.K., Babor, T.F., Korner, P., Brown, J., Bohn, M.J. Arch. Gen. Psychiatry (1994) [Pubmed]
  10. Effect of buspirone on withdrawal symptoms associated with smoking cessation. Hilleman, D.E., Mohiuddin, S.M., Del Core, M.G., Sketch, M.H. Arch. Intern. Med. (1992) [Pubmed]
  11. Serotonin receptors, buspirone, and premenstrual syndrome. Yatham, L.M., Barry, S., Dinan, T.G. Lancet (1989) [Pubmed]
  12. Effect of buspirone on prolactin secretion is not mediated by 5-HT-1a receptor stimulation. Meltzer, H.Y., Lee, H.S., Nash, J.F. Arch. Gen. Psychiatry (1992) [Pubmed]
  13. The effect of buspirone on prolactin and growth hormone secretion in man. Meltzer, H.Y., Flemming, R., Robertson, A. Arch. Gen. Psychiatry (1983) [Pubmed]
  14. Buspirone attenuates synaptic activation of hippocampal pyramidal cells. Mauk, M.D., Peroutka, S.J., Kocsis, J.D. J. Neurosci. (1988) [Pubmed]
  15. Double-blind study of adjuvant buspirone for fluoxetine-treated patients with obsessive-compulsive disorder. Grady, T.A., Pigott, T.A., L'Heureux, F., Hill, J.L., Bernstein, S.E., Murphy, D.L. The American journal of psychiatry. (1993) [Pubmed]
  16. Adjunctive buspirone in benzodiazepine treatment of four patients with panic disorder. Gastfriend, D.R., Rosenbaum, J.F. The American journal of psychiatry. (1989) [Pubmed]
  17. Combined effects of buspirone and diazepam on objective and subjective tests of performance in healthy volunteers. Mattila, M., Seppälä, T., Mattila, M.J. Clin. Pharmacol. Ther. (1986) [Pubmed]
  18. Buspirone, but not sumatriptan, induces miosis in humans: relevance for a serotoninergic pupil control. Fanciullacci, M., Sicuteri, R., Alessandri, M., Geppetti, P. Clin. Pharmacol. Ther. (1995) [Pubmed]
  19. Abuse potential of buspirone and related drugs. Balster, R.L. Journal of clinical psychopharmacology. (1990) [Pubmed]
  20. Metabolism and disposition of buspirone. Gammans, R.E., Mayol, R.F., LaBudde, J.A. Am. J. Med. (1986) [Pubmed]
  21. Investigation of the abuse liability of buspirone in alcohol-dependent patients. Griffith, J.D., Jasinski, D.R., Casten, G.P., McKinney, G.R. Am. J. Med. (1986) [Pubmed]
  22. Effects of verapamil and diltiazem on the pharmacokinetics and pharmacodynamics of buspirone. Lamberg, T.S., Kivistö, K.T., Neuvonen, P.J. Clin. Pharmacol. Ther. (1998) [Pubmed]
  23. Buspirone, a serotonin receptor agonist, increases CD4 T-cell counts and modulates the immune system in HIV-seropositive subjects. Hofmann, B., Afzelius, P., Iversen, J., Kronborg, G., Aabech, P., Benfield, T., Dybkjaer, E., Nielsen, J.O. AIDS (1996) [Pubmed]
  24. Buspirone: review of its pharmacology and current perspectives on its mechanism of action. Eison, A.S., Temple, D.L. Am. J. Med. (1986) [Pubmed]
  25. 5-Hydroxytryptamine1A and 5-hydroxytryptamine1B receptors stimulate [35S]guanosine-5'-O-(3-thio)triphosphate binding to rodent brain sections as visualized by in vitro autoradiography. Waeber, C., Moskowitz, M.A. Mol. Pharmacol. (1997) [Pubmed]
  26. Photoaffinity labeling of the 5-hydroxytryptamine 1A receptor in rat hippocampus. Ransom, R.W., Asarch, K.B., Shih, J.C. J. Neurochem. (1986) [Pubmed]
  27. Constitutive G(i2)-dependent activation of adenylyl cyclase type II by the 5-HT1A receptor. Inhibition by anxiolytic partial agonists. Albert, P.R., Sajedi, N., Lemonde, S., Ghahremani, M.H. J. Biol. Chem. (1999) [Pubmed]
  28. Obsessive-compulsive disorder, fluoxetine, and buspirone. Sternlicht, H.C. The American journal of psychiatry. (1993) [Pubmed]
  29. Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors. Peroutka, S.J. Biol. Psychiatry (1985) [Pubmed]
  30. Molecular dynamics of 5-HT1A and 5-HT2A serotonin receptors with methylated buspirone analogues. Bronowska, A., Chilmonczyk, Z., Leś, A., Edvardsen, O., Ostensen, R., Sylte, I. J. Comput. Aided Mol. Des. (2001) [Pubmed]
  31. Cytochrome P450 3A-mediated metabolism of buspirone in human liver microsomes. Zhu, M., Zhao, W., Jimenez, H., Zhang, D., Yeola, S., Dai, R., Vachharajani, N., Mitroka, J. Drug Metab. Dispos. (2005) [Pubmed]
  32. Assessing the efficacy of antianxiety agents. Rakel, R. Am. J. Med. (1987) [Pubmed]
  33. Neuroendocrine effects of buspirone in patients with generalized anxiety disorder. Cohn, J.B., Wilcox, C.S., Meltzer, H.Y. Am. J. Med. (1986) [Pubmed]
  34. Distinguishing a benzodiazepine agonist (triazolam) from a nonagonist anxiolytic (buspirone) by electroencephalography: kinetic-dynamic studies. Greenblatt, D.J., Harmatz, J.S., Gouthro, T.A., Locke, J., Shader, R.I. Clin. Pharmacol. Ther. (1994) [Pubmed]
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