Ipsapirone

Ipsapirone is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT_1A (K_i = 10 nM in hippocampal membranes).¹ It reduces 5-HT release in the rat ventral hippocampus in vivo.² Low doses of ipsapirone decrease, while high doses increase, extracellular dopamine release in the murine nucleus accumbens.³ Extracellular dopamine levels in the murine striatum increase following administration of ipsapirone at concentrations greater than 0.1 mg/kg. Ipsapirone has anxiolytic effects in vivo, inhibiting foot shock-induced aggression and passive avoidance behavior in rats (ED₅₀s = 2.2 and 0.5 mg/kg, respectively).⁴ Formulations containing ipsapirone have been used in the treatment of depression and borderline personality disorder.⁵

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1. Glaser, T., and Traber, J. Binding of the putative anxiolytic TVX Q 7821 to hippocampal 5-hydroxytryptamine (5-HT) recognition sites. Naunyn Schmiedebergs Arch. Pharmacol. 329(3), 211-215 (1985).

2. Sharp, T., Bramwell, S.R., and Grahame-Smith, D.G. 5-HT₁ agonists reduce 5-hydroxytryptamine release in rat hippocampus in vivo as determined by brain microdialysis. Br. J. Pharmacol. 96(2), 283-290 (1989).

3. Ichikawa, J., and Meltzer, H.Y. The effect of ipsapirone and S(−)-pindolol on dopamine release in rat striatum and nucleus accumbens. Brain Res. 842(2), 445-451 (1999).

4. Traber, J., Davies, M.A., Dompert, W.U., et al. Brain serotonin receptors as a target for the putative anxiolytic TVX Q 7821. Brain Res. Bull. 12(6), 741-744 (1984).

5. Rausch, J.L., Johnson, M.E., Kasik, K.E., et al. Temperature regulation in depression: Functional 5HT1A receptor adaptation differentiates antidepressant response. Neuropsychopharmacology 31(10), 2274-2280 (2006).