BACKGROUND Ziprasidone (Zeldox) is a novel antipsychotic with a unique combination of antagonist activities at monoaminergic receptors and transporters and potent agonist activity at serotonin 5-HT(1A) receptors. 5-HT(1A) receptor agonism may be an important feature in ziprasidone's clinical actions because 5-HT(1A) agonists increase cortical dopamine release, which may underlie efficacy agains...

Orer HS, Gebber GL, Barman SM. Role of serotonergic input to the ventrolateral medulla in expression of the 10-Hz sympathetic nerve rhythm. Am J Physiol Regul Integr Comp Physiol 294: R1435–R1444, 2008. First published March 12, 2008; doi:10.1152/ajpregu.00012.2008.—We studied the changes in inferior cardiac sympathetic nerve discharge (SND) produced by unilateral microinjections of 5-hydroxytr...

There is considerable evidence from research in neonatal and adult rat and mouse preparations to warrant the conclusion that activation of 5-HT2 and 5-HT1A/7 receptors leads to activation of the spinal cord circuitry for locomotion. These receptors are involved in control of locomotor movements, but it is not clear how they are implicated in the responses to 5-HT agonists observed after spinal ...

We have discovered a novel type of orally active prodrug of a dopaminergic catecholamine. The prodrug has an enone structure that by an enantioselective bioactivation is converted to the known potent mixed dopamine D1/D2 receptor agonist 5,6-di-OH-DPAT (Figure 2.1). The bioactivation mechanism was found to be selective for 2.3a ((S)-PD148903) which produces the catecholamine (S)-5,6-dihydroxy-2...

Serotonin (5HT) is crucial to normal reflex vagal modulation of heart rate (HR). Reduced baroreflex sensitivity (sBRS) and HR variability (HRV) reflect impaired neural, particularly vagal, control of HR and are independently associated with depression. In conscious, telemetered Flinders-Sensitive Line rats (FSL), a well-validated animal model of depression, we tested the hypothesis that cardiov...

the brain. Several studies have indicated that the activation of the hypothalamic-pituitary-adrenal axis changes the serotonin (5-hydroxytryptamine, 5-HT) function in the brain. The 5-HT receptor subtypes, particularly 5-HT2A and 5-HT1A receptors, have been postulated to play an important role in the pathogenesis of depression. Some clinical studies have demonstrated increases in the number of ...

A growing body of evidence indicates a role for D(3) receptors in l-DOPA-induced dyskinesias. This involvement could be amenable to non-invasive in vivo analysis using functional neuroimaging. With this goal, we examined the hemodynamic response to the dopamine D(3)-preferring agonist 7-hydroxy-N,N-di-n-propyl-2 aminotetralin (7-OHDPAT) in naïve, parkinsonian and l-DOPA-treated, dyskinetic rode...

Using extracellular recording we studied changes in the reactivity of rat frontal cortical slices to the 5-HT1A, 5-HT2 and 5-HT4 receptor agonists, (±)-2dipropyloamino-8-hydroxy-1,2,3,4-tetrahydronaphtalene hydrobromide (8-OHDPAT), (±)-2,5-dimethoxy-4-iodoamphetamine hydrochloride (DOI) and zacopride, respectively, induced by an earlier treatment of animals with corticosterone lasting 1 or 3 we...

During the last 30 years there have been many attempts to develop animal models of obsessive-compulsive disorder (OCD). Most models have not been studied further following the original publication, and in the past few years, most papers present studies employing a few established animal models, exploring the neural basis of compulsive behavior and developing new treatment strategies. Here we su...