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Last update 08 May 2025

5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

Last update 08 May 2025

Basic Info

Drugs associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

Eltoprazine Hydrochloride

Target

5-HT1A receptor x 5-HT1B receptor x 5-HT2C receptor

Mechanism

5-HT1A receptor antagonists [+2]

Active Org.

Amarantus Bioscience Holdings, Inc. [+1]

Originator Org.

Psychogenics, Inc.

Active Indication

Attention Deficit Disorder With Hyperactivity [+2]

Inactive Indication

Aggression [+3]

Drug Highest PhasePhase 3

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

EUCTR2015-000373-13-DE

/ Not yet recruitingNot Applicable

Phase 2, multicenter, randomized, double-blind, placebo-controlled, four-period cross-over, dose-range finding study to evaluate the safety, tolerability and efficacy of Eltoprazine in the treatment of levodopa induced dyskinesia in patients with Parkinson's disease.

Start Date18 Aug 2015

Sponsor / Collaborator

Amarantus Bioscience Holdings, Inc.

NCT02439125

/ Unknown statusPhase 2

Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled, 4-way Crossover, Dose-finding Study, of Eltoprazine Safety, Tolerability and Efficacy in the Treatment of Levodopa-induced Dyskinesia in Patients With Parkinson's Disease

The purpose of this study is to evaluate the safety, tolerability and efficacy of eltoprazine to treat levodopa-induced dyskinesia in patients with Parkinson's disease

Start Date01 May 2015

Sponsor / Collaborator

Amarantus Bioscience Holdings, Inc.

NCT01266174

/ CompletedPhase 2

Randomized, Double-blind, Parallel Trial Comparing the Effects of Eltoprazine (Adjunct to Anti-psychotics) With Placebo in Adults With Schizophrenia, in Improving One or More Dimensions of Cognitive Impairment Associated With Schizophrenia

The purpose of this study is to determine if eltoprazine (as an adjunct to anti-psychotic medication) improves one or more aspects of cognitive impairment in adult schizophrenic patients.

Start Date01 Aug 2011

Sponsor / Collaborator

Amarantus Bioscience Holdings, Inc.

100 Clinical Results associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

100 Translational Medicine associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

0 Patents (Medical) associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

188

Literatures (Medical) associated with 5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

01 Mar 2025·3 Biotech

Exploring therapeutic potential of Bacopa monnieri bioactive compounds against Alzheimer’s and Parkinson’s diseases

Article

Author: Singh, Sangeeta ; Shukla, Richa ; Mishra, Krishna

Parkinson's disease (PD) and Alzheimer's disease (AD) consist of progressive illnesses of central nervous system that primarily affect the elderly and are characterized by movement symptoms, memory decline, and cognitive impairment. A number of variables, including the lack of a novel treatment, a steady rise in the patient population, and the high expense of care and treatment, have contributed to the growing significance of these diseases. In recent decades, we have gained a better understanding of the causes of diseases, but complex mechanisms of neuronal loss, combined with physiological factors that are incompatible, pose challenges in describing the pathogenic processes and devising effective treatments. Currently, there are no known treatments for most of these diseases, rendering them incurable. Therefore, there is a pressing need for therapeutic interventions that have the potential to effectively treat neurodegeneration. This study aimed to evaluate the efficacy of the ayurvedic herb Bacopa monnieri bioactive components against the therapeutic targets HTR1A, HTR1B, HTR2A, HTR2C, HTR7, alpha-synuclein, amyloid beta, and tau protein of Alzheimer's and Parkinson's illnesses. The docking analysis revealed the promising binding affinity with Quercetin, Apigenin, and Luteolin and Molecular mechanics/generalized Born surface area (MM/GBSA) further confirmed the stability of the complexes. In vitro investigation indicated that Quercetin is the most effective for treating AD and PD due to its considerable inhibition of alpha-synuclein production, whereas Luteolin is the favorable one for preventing both diseases by mitigating effects during Rotenone treatment. The future implications and constraints of the current study suggest that further validation in Invivo models of Alzheimer's and Parkinson's diseases is necessary to investigate the effects of Quercetin and Apigenin in the treatment of these conditions, as well as Luteolin and Quercetin for their prevention.Supplementary InformationThe online version contains supplementary material available at 10.1007/s13205-025-04224-6.

14 Sep 2023·ACS Medicinal Chemistry Letters

Exploring Next-Generation Therapeutics: Morphic Mixtures and Specified Salts for the Treatment of Mental Disorders and CNS Modulation

Author: Kargbo, Robert B.

This Patent Highlight delves into the potential of next-generation therapeutics for treating mental disorders and modulating the central nervous system (CNS). Among the serotonin receptor subtypes, 5-HT2A, 5-HT2C, 5-HT1A, and 5-HT1B have shown promise in CNS disorder treatment. Approved drugs targeting these receptors, such as antipsychotics and psychedelics, provide valuable insights into their therapeutic effects. However, modulation of these receptors can lead to side effects like hallucinations and altered perception. The development of 5-HT2A agonists with minimized mood changes and improved therapeutic benefits is crucial. Furthermore, exploring morphic salt mixtures and specified salts offers innovative approaches to effectively modulating CNS activity and treating mental disorders.

01 Mar 2023·European Archives of Psychiatry and Clinical Neuroscience

Elevated levels of serotonin 5-HT2A receptors in the orbitofrontal cortex of antisocial individuals

Article

Author: Braccagni, Giulia ; Scheggi, Simona ; Bortolato, Marco

Antisocial behavior (ASB) is characterized by frequent violations of the rights and properties of others, as well as aggressive conduct. While ample evidence points to a critical role of serotonin in the emotional modulation of social responses, the implication of this neurotransmitter in ASB is unclear. Here, we performed the first-ever postmortem analysis of serotonergic markers in the orbitofrontal cortex (OFC) of male subjects with ASB (n = 9). We focused on this brain region, given its well-recognized role in social response and ASB pathophysiology. Given that all individuals also had a substance use disorder (SUD) diagnosis, two age-matched control groups were used: SUD only and unaffected controls. Tissues were processed for immunoblotting analyses on eight key serotonergic targets: tryptophan hydroxylase 2 (TPH2), the rate-limiting enzyme of brain serotonin synthesis; serotonin transporter (SERT), the primary carrier for serotonin uptake; monoamine oxidase A (MAOA), the primary enzyme for serotonin catabolism; and five serotonin receptors previously shown to influence social behavior: 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C, and 5-HT₄. Our analyses documented a significant increase in 5-HT_2A receptor levels in the ASB + SUD group compared to SUD-only controls. Furthermore, TPH2 levels were significantly reduced in the SUD group (including SUD only and ASB + SUD) compared to unaffected controls. No difference was detected in the expression of any other serotonergic target. These results are in keeping with previous evidence showing high 5-HT_2A receptor binding in the OFC of pathologically aggressive individuals and point to this molecule as a potential target for ASB treatment.

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5-HT1A receptor x 5-HT2C receptor x 5-HT1B receptor

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