Asenapine elevates cortical dopamine, noradrenaline and serotonin release. Evidence for activation of cortical and subcortical dopamine systems by different mechanisms

Olivia FrånbergT H Svensson


Asenapine, a psychopharmacologic agent developed for schizophrenia and bipolar disorder, has higher affinity for 5-HT(2A/C,6,7) and alpha(2) adrenergic receptors than for D(2) receptors. Asenapine exhibits potent antipsychotic-like effects without inducing catalepsy, increases cortical and subcortical dopamine release, and facilitates cortical glutamatergic transmission in rats. In this study, we further analyzed the effects of asenapine on dopaminergic, noradrenergic, and serotonergic systems in the rat brain. We studied the effects of asenapine on (1) dopaminergic neurons in the ventral tegmental area (VTA) and noradrenergic neurons in the locus coeruleus using in vivo single cell recording, (2) release of dopamine and noradrenaline (medial prefrontal cortex), serotonin (frontal cortex), and dopamine (nucleus accumbens), using in vivo microdialysis. Systemic asenapine increased dopaminergic (0.001-0.2 mg/kg, i.v.) and noradrenergic (0.025-0.05 mg/kg i.v.) neuronal firing, and asenapine (0.1-0.2 mg/kg, s.c) increased cortical noradrenaline and serotonin output. Local asenapine administration increased all three monoamines in the cortex but did not affect accumbal dopamine output. Intra-VTA tetrodotoxin perfusion blocked asenap...Continue Reading


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