Last update 01 Nov 2024

D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

Last update 01 Nov 2024

Basic Info

Drugs associated with D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

LEK-8829

Target

5-HT1A receptor x 5-HT2A receptor x D1 receptor x D2 receptor

Mechanism

5-HT1A receptor antagonists [+3]

Active Org.-

Originator Org.

Lek Pharmaceuticals dd

Active Indication-

Inactive Indication

Parkinson Disease

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

100 Translational Medicine associated with D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

0 Patents (Medical) associated with D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

Literatures (Medical) associated with D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

01 Nov 2022·Food and Chemical Toxicology

Neurotoxicity induced by the pyrethroid lambda-cyhalothrin: Alterations in monoaminergic systems and dopaminergic and serotoninergic pathways in the rat brain

Article

Author: Maximiliano, Jorge-Enrique ; Ares, Irma ; Martínez, Marta ; Martínez-Larrañaga, María-Rosa ; Lopez-Torres, Bernardo ; Anadón, Arturo ; Martínez, María-Aránzazu

The effects of Type II pyrethroid lambda-cyhalothrin on dopamine (DA) and serotonin (5-HT) synthesis in rat brain regions (striatum, hippocampus, prefrontal cortex, hypothalamus and midbrain) were studied. Lambda-cyhalothrin (1, 4 and 8 mg/kg bw, oral gavage, 6 days) induced a decrease of DA, 5-HT and metabolites contents, in a brain regional- and dose-related manner. The major decreases in DA and 5-HT contents were observed in hippocampus and prefrontal cortex tissues. This research study also showed in hippocampus and prefrontal cortex, that lambda-cyhalothrin modified the mRNA levels of DA transporter gene (Dat1 up-regulation), 5-HT transporter gene (SERT down-regulation), DA receptor genes (Drd1and Drd2 down-regulation), 5-HT receptor genes (5-HT1A and 5-HT2A down-regulation/up-regulation), DA synthesis gene (TH down-regulation), 5-HT synthesis gene (TPH2 down-regulation), DA and 5-HT degradation genes (MAOA and MAOB up-regulation). These results reveal that lambda-cyhalothrin altered central nervous system (CNS) monoaminergic neurotransmitters. Lambda-cyhalothrin evoked a selective neurotoxic injury to dopaminergic and serotoninergic pathways. These findings may clarify on the pyrethroids-induced neurotoxicity mechanisms and could involve pyrethroids as environmental risk factors leading to the development of neurodegenerative diseases.

01 Dec 2019·Progress in Neuro-Psychopharmacology and Biological PsychiatryQ2 · MEDICINE

Differential expression of synaptic markers regulated during neurodevelopment in a rat model of schizophrenia-like behavior

Q2 · MEDICINE

Article

Author: Fernandez-Teruel, Alberto ; Sanchez-Gonzalez, Ana ; Elfving, Betina ; Aznar, Susana ; Tobeña, Adolf ; Rio-Alamos, Cristobal ; Müller, Heidi Kaastrup ; Østerbøg, Tina Becher ; Oliveras, Ignasi

Schizophrenia is considered a neurodevelopmental disorder. Recent reports relate synaptic alterations with disease etiology. The inbred Roman High- (RHA-I) and Low- (RLA-I) Avoidance rat strains are a congenital neurobehavioral model, with the RHA-I displaying schizophrenia-related behaviors and serotonin 2A (5-HT2A) and metabotropic glutamate 2 (mGlu2) receptor alterations in the prefrontal cortex (PFC). We performed a comprehensive characterization of the RHA-I/RLA-I rats by real-time qPCR and Western blotting for 5-HT1A, 5-HT2A, mGlu2, dopamine 1 and dopamine 2 receptors (DRD1 and DRD2), AMPA receptor subunits Gria1, Gria2 and NMDA receptor subunits Grin1, Grin2a and Grin2b, as well as pre- and post-synaptic components in PFC and hippocampus (HIP). Besides corroborating decreased mGlu2 (Grm2) expression, we found increased mRNA levels for Snap25, Synaptophysin (Syp), Homer1 and Neuregulin-1 (Nrg1) in the PFC of the RHA-I and decreased expression of Vamp1, and Snapin in the HIP. We also showed alterations in Vamp1, Grin2b, Syp, Snap25 and Nrg1 at protein levels. mRNA levels of Brain Derived Neurotrophic Factor (BDNF) were increased in the PFC of the RHA-I rats, with no differences in the HIP, while BDNF protein levels were decreased in PFC and increased in HIP. To investigate the temporal dynamics of these synaptic markers during neurodevelopment, we made use of the open source BrainCloud™ dataset, and found that SYP, GRIN2B, NRG1, HOMER1, DRD1 and BDNF expression is upregulated in PFC during childhood and adolescence, suggesting a more immature neurobiological endophenotype in the RHA-I strain.

01 Jan 2018·Brain and BehaviorQ4 · PSYCHOLOGY

Maternal separation affects expression of stress response genes and increases vulnerability to ethanol consumption

Q4 · PSYCHOLOGY

ArticleOA

Author: Correia, Diego ; de Almeida Magalhães, Taciani ; Damasceno, Samara ; de Carvalho, Luana Martins ; Brunialti Godard, Ana Lúcia

AbstractIntroductionMaternal separation is an early life stress event associated with behavioral alterations and ethanol consumption. We aimed to expand the current understanding on the molecular mechanisms mediating the impact of postnatal stress on ethanol consumption.MethodsIn the first experiment (T1), some of the pups were separated from their mothers for 6 hr daily (Maternal Separation group ‐ MS), whereas the other pups remained in the cage with their respective mothers (Control group ‐ C). In the second experiment (T2), mice from both groups were subjected to the model of free‐choice between water and sucrose solution or between water and ethanol solution. Maternal behavior was assessed at the end of T1. At the end of both T1 and T2, pups were subjected to the light/dark box behavioral test and blood corticosterone concentrations were analyzed.ResultsOur maternal separation protocol led to intense maternal care and affected weight gain of the animals. The expression of stress response genes was altered with higher levels of Crh and Pomc being observed in the hypothalamus, and higher levels of Crhr1, Crhr2, Htr2a and lower levels of Nr3c1 and Htr1a being observed in the hippocampus after T1. At the end of T2, we observed higher levels of Avp and Pomc in the hypothalamus, and higher levels of Crhr1, Crhr2, Nr3c1, Slc6a4, Bdnf and lower levels of Htr1a in the hippocampus. Additionally, maternal separation increased vulnerability to ethanol consumption during adolescence and induced changes in anxiety/stress‐related behavior after T2. Furthermore, voluntary ethanol consumption attenuated stress response and modified expression of reward system genes: enhancing Drd1 and Drd2, and reducing Gabbr2 in the striatum.ConclusionMaternal separation induced behavioral changes and alterations in the expression of key genes involved in HPA axis and in the serotonergic and reward systems that are likely to increase vulnerability to ethanol consumption in adolescence. We demonstrated, for the first time, that ethanol consumption masked stress response by reducing the activity of the HPA axis and the serotonergic system, therefore, suggesting that adolescent mice from the MS group probably consumed ethanol for stress relieving purposes.

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D1 receptor x 5-HT1A receptor x D2 receptor x 5-HT2A receptor

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