The effects of azapirones on serotonin1A neurons of the dorsal raphe

Paroxetine administration to influence human exercise capacity, perceived effort or hormone responses during prolonged exercise in a warm environment

“…The failure of paroxetine administration to influence the circulating concentration of prolactin or cortisol raises questions concerning the role of 5‐HT in their secretion during exercise. Both pre‐ and postsynaptic 5‐HT receptors are involved in the regulation of cortisol secretion (Van de Kar, 1997) but activation of somatodendritic 5‐HT 1a autoreceptors on the 5‐HT cells in the dorsal raphe nuclei during stressful events may limit cortisol secretion (Matheson et al 1994). Furthermore, species‐dependent terminal 5‐HT 1b/d autoreceptors regulate the volume of 5‐HT released into the synaptic cleft (*).…”

Differential Effects of Ipsapirone on 5‐Hydroxytryptamine Release in the Dorsal and Median Raphe Neuronal Pathways

“…Assuming that the 5-HT LA receptor subtype represents a single receptor class (Albert et al, 1990;Radja et al, 1992), the regional selectivity of ipsapirone is not easy to explain, although some tentative explanations can be advanced. Ipsapirone behaves as a full agonist at dorsal raphe 5-HTIA receptors, as judged by the complete suppression of cell firing induced by this agent Aghajanian, 1987, 1988;Haj-Dahmane et al, 1991;Cox et al, 1993;Matheson et al, 1994). The large 5-HI decrease elicited by 10 mg/kg ipsapirone in frontal cortex or striatum is also indicative of a full agonistic interaction with 5-HILA autoreceptors in dorsal raphe neurons.…”

Azapirone 5-HT1A receptor partial agonist treatment for major depressive disorder: systematic review and meta-analysis

“…The azapirone anxiolytic drugs (buspirone, gepirone, ipsapirone, tandospirone and zalospirone), which function as 5-HT 1A receptor partial agonists, are frequently used as adjunctive treatments for MDD patients with inadequate response to first-line antidepressant drugs (Matheson et al 1994; Newman-Tancredi & Kleven, 2011). We identified 15 randomized controlled trials (RCTs) comparing 5-HT 1A agonists with placebo: four studies with buspirone (Fabre, 1990; Rickels et al 1990; Schweizer et al 1998; Fabre et al 2012), seven with gepirone (Jenkins et al 1990; Rausch et al 1990; McGrath et al 1994; Feiger, 1996; Wilcox et al 1996; Feiger et al 2003; Bielski et al 2008), three with ipsapirone (Heller et al 1990; Lapierre et al 1998; Stahl et al 1998) and one with zalospirone (Rickels et al 1996).…”