The therapeutic potential of 5-HT1A receptors: a patent review

Lacivita, Enza; Pilato, Pantaleo Di; Giorgio, Paola De; Colabufo, Nicola Antonio; Berardi, Francesco; Perrone, Roberto; Leopoldo, Marcello

doi:10.1517/13543776.2012.703654

Cited by 38 publications

(24 citation statements)

References 49 publications

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“…thus, our results suggest that 8-OH-DPAt at high dose might be useful not only in the control of epileptic seizures but also in the comorbid memory impairments which occur not infrequently in patients with epilepsy, especially with tLE (Bell et al 2011). these positive cognitive effects together with the possible antidepressant properties of 5-Ht 1A agonists including 8-OH-DPAt (Lacivita et al 2008) and the antiepileptic activity shown here may offer new therapeutic possibilities (Lacivita et al 2012) for an old drug.…”

Section: Discussionmentioning

confidence: 55%

High dose of 8-OH-DPAT decreases maximal dentate gyrus activation and facilitates granular cell plasticity in vivo

et al. 2013

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plasticity was studied. Rats injected with 8-OH-DPAt exhibited a significant reduction in MDA and epileptic discharges, a decrease in paired-pulse facilitation and an increase in long-term potentiation. this study suggests that 8-OH-DPAt or in general 5-Ht 1A/7 agonists might be useful for the treatment of tLE and also have some beneficial effects on the comorbid cognitive disorders seen in epileptic patients.

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Section: Discussionmentioning

confidence: 55%

High dose of 8-OH-DPAT decreases maximal dentate gyrus activation and facilitates granular cell plasticity in vivo

et al. 2013

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“…A study conducted in the United States (US) indicated that approximately 50%-70% of American people have been exposed to traumatic events such as earthquakes, terrorism, warfare and violent personal assault, with 5%-12% of them developing an anxiety like PTSD during their life time [1, 2]. PTSD is characterized by nightmares, flashbacks, mood swings, psychological/physical distress and hyper-arousal [3, 4].…”

Section: Introductionmentioning

confidence: 99%

“…Both hippocampus and amygdala are major brain regions that respond to anxiogenesis and stress stimuli [1, 5]. The pathophysiology of PTSD is attributed to dysfunction of the hippocampus and amygdala, whose activity is associated with stress-related emotional arousal [6, 7].…”

Section: Introductionmentioning

confidence: 99%

Stimulation of Anxiety-Like Behavior via ERK Pathway by Competitive Serotonin Receptors 2A and 1A in Post-Traumatic Stress Disordered Mice

Xiang

Jiang

et al. 2017

Neurosignals

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Background/Aims: Serotonin 5HT2A and 5HT1A receptors (5HT2AR, 5HT1AR) have the closest connection to anxiety-like behavior in post-traumatic stress disorder (PTSD). However, the underlying mechanism remains unclear. In this study, we explored the connection between 5HT2A and 5HT1A receptors and anxiety-like behavior. Methods: In the PTSD animal model, mice were exposed to conditioned fear stress coupled with single-prolonged stress (CF+SPS). Post stress infliction and behavioral tests, of which include open field, freezing behavior and elevated plus maze tests were carried out to examine establishment of the proposed model. Both Western blot analysis and immunofluorescence labeling were used to evaluate protein expressions of 5HT2AR, 5HT1AR, ERK1, ERK2 and c-Myc in the hippocampi of the mice and RT Q-PCR was employed for evaluation of the relative mRNA expressions. Results: Based on the model established utilizing the CF+SPS procedure, we found 5HT2AR to play a positive role on anxiety-like behavior by inhibiting the expression of 5HT1AR. In addition, the ERK-c-Myc pathway elicited the effect of 5HT2AR and 5HT1AR on anxiety-like behavior in PTSD, 5-HT enhanced the anxiety-like behavior through both 5HT2AR and 5HT1AR. Conclusion: These findings suggest competive interaction between 5HT2AR and 5HT1AR actively affects anxiety-like behavior in the hippocampi of PTSD mice via the ERK pathway.

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“…Furthermore, it is known that DMT act as an agonist at 5-HT 1A receptors 8,70 . The activation of 5-H 1A receptors may be in the basis of neurogenesis in the hippocampus and in the prefrontal cortex and its activation seems to be in the basis of the antidepressant effects of antidepressive drugs 71 .…”

Section: Suggestions For Future Researchmentioning

confidence: 99%

Ayahuasca: what mental health professionals need to know

Santos

Bouso²,

Hallak

2017

Arch. Clin. Psychiatry (São Paulo)

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Background: Ayahuasca is a psychoactive ethnobotanical concoction that has been used for decades by indigenous groups of the Northwestern Amazon and by syncretic religious organizations for ritual and therapeutic purposes. In the last two decades, it is being used worldwide in evolving practices. Ayahuasca seem to therapeutic effects, but controlled studies are lacking. Moreover, its safety and toxicity are not completely understood. Objectives: To present an overview of the effects of ayahuasca based on the most recent human studies. Methods: Narrative review. Results: Ayahuasca administration in controlled settings appears to be safe from a subjective and physiological perspective, with few adverse reactions being reported. More frequent adverse reactions occur in non-controlled settings. Prolonged psychotic reactions are rare and seem to occur especially in susceptible individuals. Ayahuasca showed antidepressive, anxiolytic, and antiaddictive effects in animal models, observational studies, and in open-label and controlled studies. Discussion: Ayahuasca administration in controlled settings appear to be safe. Moreover, ayahuasca seem to have therapeutic effects for treatment-resistant psychiatric disorders that should be further investigated in randomized controlled clinical trials. However, medical complications and cases of prolonged psychotic reactions have been reported, and people with personal or family history of psychotic disorders should avoid ayahuasca intake.

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The therapeutic potential of 5-HT1A receptors: a patent review

Cited by 38 publications

References 49 publications

High dose of 8-OH-DPAT decreases maximal dentate gyrus activation and facilitates granular cell plasticity in vivo

High dose of 8-OH-DPAT decreases maximal dentate gyrus activation and facilitates granular cell plasticity in vivo

Stimulation of Anxiety-Like Behavior via ERK Pathway by Competitive Serotonin Receptors 2A and 1A in Post-Traumatic Stress Disordered Mice

Ayahuasca: what mental health professionals need to know

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