The novel 5-HT2 receptor antagonist, RP 62203, selectively blocks serotoninergic but not dopaminergic-induced inhibition in the rat prefrontal cortex

Mantz, Jean; Głowiński, J.; Thierry, Anne‐Marie

doi:10.1016/0014-2999(91)90840-m

Cited by 7 publications

(2 citation statements)

References 9 publications

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“…5-HT 2 receptor activation also increases excitatory postsynaptic currents in rat layer V PPNs Marek 1997, 1999). In contrast, 5-HT 2 receptor activation inhibits N-methyl-D-aspartate (NMDA) receptormediated currents (Arvanov and Wang 1998;Arvanov et al 1999a;Arvanov et al 1999b) and spontaneous activity (Bergqvist et al 1999;Godbout et al 1991;Mantz et al 1990). Furthermore, 5-HT 2 receptor blockade with atypical neuroleptics induces PFC immediate early genes (Robertson and Fibiger 1996;Robertson et al 1994;Wiesel et al 1994).…”

Section: Introductionmentioning

confidence: 99%

Stimulation of 5-HT₂Receptors in Prefrontal Pyramidal Neurons Inhibits Ca_v1.2 L-Type Ca²⁺Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Day

Olson

Platzer³

et al. 2002

Journal of Neurophysiology

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There is growing evidence linking alterations in serotonergic signaling in the prefrontal cortex to the etiology of schizophrenia. Prefrontal pyramidal neurons are richly innervated by serotonergic fibers and express high levels of serotonergic 5-HT(2)-class receptors. It is unclear, however, how activation of these receptors modulates cellular activity. To help fill this gap, whole cell voltage-clamp and single-cell RT-PCR studies of acutely isolated layer V-VI prefrontal pyramidal neurons were undertaken. The vast majority (>80%) of these neurons had detectable levels of 5-HT(2A) or 5-HT(2C) receptor mRNA. Bath application of 5-HT(2) agonists inhibited voltage-dependent Ca(2+) channel currents. L-type Ca(2+) channels were a particularly prominent target of this signaling pathway. The L-type channel modulation was blocked by disruption of G(alphaq) signaling or by inhibition of phospholipase Cbeta. Antagonism of intracellular inositol trisphosphate signaling, chelation of intracellular Ca(2+), or depletion of intracellular Ca(2+) stores also blocked this modulation. Inhibition of the Ca(2+)-dependent phosphatase calcineurin prevented receptor-mediated modulation of L-type currents. Last, the 5-HT(2) receptor modulation was robustly expressed in neurons from Ca(v)1.3 knockout mice. These findings argue that 5-HT(2) receptors couple through G(alphaq) proteins to trigger a phospholipase Cbeta/inositol trisphosphate signaling cascade resulting in the mobilization of intracellular Ca(2+), activation of calcineurin, and inhibition of Ca(v)1.2 L-type Ca(2+) currents. This modulation and its blockade by atypical neuroleptics could have wide-ranging effects on synaptic integration and long-term gene expression in deep-layer prefrontal pyramidal neurons.

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Section: Introductionmentioning

confidence: 99%

Stimulation of 5-HT₂Receptors in Prefrontal Pyramidal Neurons Inhibits Ca_v1.2 L-Type Ca²⁺Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Day

Olson

Platzer³

et al. 2002

Journal of Neurophysiology

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“…However, a selective 5-HT2A receptor innervation from DRN may not generalize to other regions. Thus, electrophysiological experiments found that 5-HT2A receptor-mediated responses in the prefrontal cortex can be evoked by stimulation of the MRN [52]. 5-HT2A receptor subtypes couple positively to phospholipase C and lead to increased accumulation of inositol phosphates and intracellular Ca2+ via G-protein coupling [53,54].…”

Section: -Ht2a Receptormentioning

confidence: 97%

Serotonin in antipsychotic drugs action

Amato

2015

Behavioural Brain Research

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Preparation of [18F]RP 62203, a selective ligand for the study of serotonin receptors (5-HT2) by rapid “in situ” piperazine formation

Lasne

Barré

Huard

et al. 1994

Applied Radiation and Isotopes

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The novel 5-HT2 receptor antagonist, RP 62203, selectively blocks serotoninergic but not dopaminergic-induced inhibition in the rat prefrontal cortex

Cited by 7 publications

References 9 publications

Stimulation of 5-HT₂Receptors in Prefrontal Pyramidal Neurons Inhibits Ca_v1.2 L-Type Ca²⁺Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Stimulation of 5-HT₂Receptors in Prefrontal Pyramidal Neurons Inhibits Ca_v1.2 L-Type Ca²⁺Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Serotonin in antipsychotic drugs action

Preparation of [18F]RP 62203, a selective ligand for the study of serotonin receptors (5-HT2) by rapid “in situ” piperazine formation

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The novel 5-HT2 receptor antagonist, RP 62203, selectively blocks serotoninergic but not dopaminergic-induced inhibition in the rat prefrontal cortex

Cited by 7 publications

References 9 publications

Stimulation of 5-HT2Receptors in Prefrontal Pyramidal Neurons Inhibits Cav1.2 L-Type Ca2+Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Stimulation of 5-HT2Receptors in Prefrontal Pyramidal Neurons Inhibits Cav1.2 L-Type Ca2+Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Serotonin in antipsychotic drugs action

Preparation of [18F]RP 62203, a selective ligand for the study of serotonin receptors (5-HT2) by rapid “in situ” piperazine formation

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Stimulation of 5-HT₂Receptors in Prefrontal Pyramidal Neurons Inhibits Ca_v1.2 L-Type Ca²⁺Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade

Stimulation of 5-HT₂Receptors in Prefrontal Pyramidal Neurons Inhibits Ca_v1.2 L-Type Ca²⁺Currents Via a PLCβ/IP3/Calcineurin Signaling Cascade