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Anna Partyka, Magdalena Jastrzębska-Więsek, Lucyna Antkiewicz-Michaluk, Jerzy Michaluk, Agnieszka Wąsik, Vittorio Canale, Paweł Zajdel, Marcin Kołaczkowski, Anna Wesołowska
The aim of the present study was to investigate and compare the ability of three novel 5-HT6 and/or 5-HT7 receptor antagonists as follows: PZ-668-a preferential 5-HT6 antagonist; PZ-1433-a preferential 5-HT7 antagonist; and ADN-1184-a monoaminergic ligand with potent 5HT6/7 antagonist properties, to augment the effect of antidepressant drugs with different mechanisms of action (escitalopram, reboxetine, and bupropion) in the forced swim test in rats. In neurochemical ex vivo experiments, the influence of the tested compounds on levels of monoamines and their metabolites were determined in the rat frontal cortex, in addition to behavioral experiments...
October 9, 2018: Behavioural Brain Research
Arvind Kumar, Harpreet Singh, Amrita Mishra, Arun K Mishra
OBJECTIVE: Aripiprazole,a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole. DEVELOPMENT: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S. Food and Drug Administration (USFDA) in the end months of 2002 to with an aim to treat patients with schizophrenia...
October 8, 2018: Current Drug Discovery Technologies
Hyung Gon Lee, Ji A Song, Dong Soo Han, Kyeong Wan Woo, Myung Ha Yoon
This study examined the effects of intrathecal areca nut on spinal nerve-ligated and chemotherapy-induced neuropathic pain (NP), and investigated the relevance of spinal 5-hydroxytryptamine (5-HT) and α2-adrenergic receptors to those effects. For drug administration, intrathecal catheters were inserted into the subarachnoid space of male Sprague-Dawley rats. NP was induced either by spinal nerve ligation (left spinal nerves L5 and L6) or by chemotherapeutic injection (intraperitoneal cisplatin, 2 mg/kg/day, once daily for 4 days)...
October 10, 2018: Pharmacology
Anna Rita Zuena, Daniela Maftei, Giovanni Sebastiano Alemà, Francesca Dal Moro, Roberta Lattanzi, Paola Casolini, Ferdinando Nicoletti
Vortioxetine is a multimodal antidepressant that potently antagonizes 5-HT3 serotonin receptors, inhibits the high affinity serotonin transporter, activates 5-HT1A and 5-HT1B receptors, and antagonizes 5-HT1D and 5-HT7 receptors. 5-HT3 receptors largely mediate the hyperalgesic activity of serotonin that occurs in response to nerve injury. Activation of 5-HT3 receptors contributes to explain why selective serotonin reuptake inhibitors, such as fluoxetine, are not indicated in the treatment of neuropathic pain...
October 5, 2018: Molecular Pain
Joanna Sowa, Magdalena Kusek, Marcin Siwiec, Joanna Ewa Sowa, Bartosz Bobula, Krzysztof Tokarski, Grzegorz Hess
RATIONALE: Chronic stress and corticosterone have been shown to affect serotonin (5-HT) neurotransmission; however, the influence of stress on the activity of the dorsal raphe nucleus (DRN), the main source of 5-HT in the forebrain, is not well understood. In particular, it is unknown if and how stress modifies DRN 5-HT7 receptors, which are involved in the modulation of the firing of local inhibitory interneurons responsible for regulating the activity of DRN projection cells. OBJECTIVES: Our study aimed to investigate the effect of repeated corticosterone injections on the modulation of the inhibitory transmission within the DRN by 5-HT7 receptors and whether it could be reversed by treatment with a 5-HT7 receptor antagonist...
September 28, 2018: Psychopharmacology
Ahmad Arbabi Jahan, Abolfazl Rad, Mustafa Ghanbarabadi, Bahareh Amin, Mohammad Mohammad-Zadeh
AIM: Curcumin, derived from turmeric, has been demonstrated to be effective in controlling seizures, although the exact mechanism is yet unknown. In this study, the role of serotonin and its receptors in the anticonvulsant effect of curcumin was evaluated in mice. MAIN METHODS: Total 110 mice were randomly divided into 11 groups (n = 10). In the first to the fourth groups, the role of curcumin (150 mg/kg, i.p) and serotonin (PCPA (100 mg/kg); was used to deplete the brain serotonin levels) was investigated...
October 15, 2018: Life Sciences
T E Schwasinger-Schmidt, M Macaluso
This chapter addresses the following FDA-approved medications for the treatment of major depressive disorder available for use in the United States including bupropion, mirtazapine, trazodone, vortioxetine, and vilazodone. These medications do not belong to one of the previously featured classes of antidepressants discussed in the preceding chapters. Each medication featured in this chapter has a unique structure and properties that target diverse receptors in the central nervous system. These diverse targets are distinct from other classes of medications used to treat major depressive disorder...
September 8, 2018: Handbook of Experimental Pharmacology
Rafał Kurczab, Vittorio Canale, Grzegorz Satała, Paweł Zajdel, Andrzej J Bojarski
A computational approach combining a structure-activity relationship library of halogenated and the corresponding unsubstituted ligands (called XSAR) with QM-based molecular docking and binding free energy calculations was used to search for amino acids frequently targeted by halogen bonding (hot spots) in a 5-HT7 R as a case study. The procedure identified two sets of hot spots, extracellular (D2.65, T2.64, and E7.35) and transmembrane (C3.36, T5.39, and S5.42), which were further verified by a synthesized library of halogenated arylsulfonamide derivatives of (aryloxy)ethylpiperidines...
September 21, 2018: Journal of Medicinal Chemistry
Krzysztof Miazga, Hanna Fabczak, Ewa Joachimiak, Małgorzata Zawadzka, Łucja Krzemień-Ojak, Marek Bekisz, Anna Bejrowska, Larry M Jordan, Urszula Sławińska
Serotonin (5-hydroxytryptamine; 5-HT) plays an important role in control of locomotion, partly through direct effects on motoneurons. Spinal cord complete transection (SCI) results in changes in 5-HT receptors on motoneurons that influence functional recovery. Activation of 5-HT2A and 5-HT7 receptors improves locomotor hindlimb movements in paraplegic rats. Here, we analyzed the mRNA of 5-HT2A and 5-HT7 receptors (encoded by Htr2a and Htr7 genes, resp.) in motoneurons innervating tibialis anterior (TA) and gastrocnemius lateralis (GM) hindlimb muscles and the tail extensor caudae medialis (ECM) muscle in intact as well as spinal rats...
2018: Neural Plasticity
A N Tamvacakis, A Senatore, P S Katz
The marine mollusc, Pleurobranchaea californica varies daily in whether it swims and this correlates with whether serotonin (5-HT) enhances the strength of synapses made by the swim central pattern generator neuron, A1/C2. Another species, Tritonia diomedea , reliably swims and does not vary in serotonergic neuromodulation. A third species, Hermissenda crassicornis , never produces this behaviour and lacks the neuromodulation. We found that expression of particular 5-HT receptor subtype (5-HTR) genes in single neurons correlates with swimming...
August 22, 2018: Proceedings. Biological Sciences
Xiaozhen Yang, Genyong Huang, Minjie Xu, Cong Zhang, Yongxu Cheng
Serotonin (5-HT) regulates numerous physiological functions and processes, such as light adaptation, food intake and ovarian maturation, and plays the role through 5-HT receptors. To our knowledge, this is the first study to isolate and characterize the serotonin receptor 7 (5-HT7 receptor) cDNA encoded in Eriocheir sinensis, an economically important aquaculture species in China, by performing rapid-amplification of cDNA ends. The full-length of 5-HT7 receptor gene cDNA is 2328 bp and encodes a polypeptide with 590 amino acids that are highly homologous with other crustaceans 5-HT7 receptor genes...
December 2018: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
Katarzyna Kucwaj-Brysz, Rafał Kurczab, Ewa Żesławska, Annamaria Lubelska, Małgorzata Anna Marć, Gniewomir Latacz, Grzegorz Satała, Wojciech Nitek, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
In order to search for active and selective serotonin 5-HT7 R antagonists among 3,5-disubstituted arylpiperazine-imidazolidine-2,4-diones, the role of the introduction/deletion and the mutual orientation of aromatic rings was analyzed. Chemical modifications of 2nd generation lead structure of 3-(3-(4-(diphenylmethyl)piperazin-1-yl)-2-hydroxypropyl)-5-(4-fluorophenyl)-5-methylimidazolidine-2,4-dione ( 2 , KKB16) were performed. New derivatives ( 4-18 ) were designed and synthesized. X-ray crystallographic analysis of the representative compound 5-(4-fluorophenyl)-3-[2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl]-5-methylimidazolidine-2,4-dione ( 3 ) was performed to support molecular modeling and SAR studies...
June 1, 2018: MedChemComm
Toshie Kaizuka, Takashi Hayashi
BACKGROUND: In the vertebrate central nervous system as well as in the periphery, serotonin, also known as 5-hydroxytriptamine (5-HT), function as a neurotransmitter, a hormone or a mitogen. 5-HT receptors are composed of 7 family 5-HT1-7 receptors, comprising of 14 structurally and pharmacologically distinct 5-HT receptor subtypes. Previous experimental studies showed that mouse 5-HT1A , 5-HT4 and 5-HT7 receptors are regulated by post-translational protein palmitoylation, the reversible attachment of the lipid palmitate to intracellular cysteine residues...
June 2018: Neuropsychopharmacology reports
Meysam Amidfar, Yong-Ku Kim
Conventional serotonin-enhancing antidepressants including selective serotonin reuptake inhibitors (SSRIs) and serotonin and norepinephrine reuptake inhibitors (SNRIs) have shown effectiveness in the treatment of major depression, but their significant limitations such as slowness of action have led to intensive research efforts to develop new antidepressants. Increased synaptic neurotransmission of serotonin (5-hdroxytryptamine; 5-HT) through orchestration of stimulation and blockade of various subtypes of 5-HT receptors is involved in the mechanisms of action of SSRIs...
August 2, 2018: Current Pharmaceutical Design
Mei Huang, Sunoh Kwon, Lakshmi Rajagopal, Wenqi He, Herbert Y Meltzer
RATIONALE: The effect of atypical antipsychotic drugs (AAPDs), e.g., lurasidone, to improve cognitive impairment associated with schizophrenia (CIAS), has been suggested to be due, in part, to enhancing release of dopamine (DA), acetylcholine (ACh), and glutamate (Glu) in cortex and hippocampus. RESULTS: The present study found acute lurasidone reversed the cognitive deficit in novel object recognition (NOR) in subchronic (sc) phencyclidine (PCP)-treated mice, an animal model for CIAS...
October 2018: Psychopharmacology
Kevin M Blattner, Daniel J Canney, Douglas A Pippin, Benjamin E Blass
It is well-documented that serotonin (5-HT) exerts its pharmacological effects through a series of 5-HT receptors. The most recently identified member of this family, 5-HT7 , was first identified in 1993. Over the course of the last 25 years, this receptor has been the subject of intense investigation, and it has been demonstrated that 5-HT7 plays an important role in a wide range of pharmacological processes. As a result of these findings, modulation of 5-HT7 activity has been the focus of numerous drug discovery and development programs...
September 4, 2018: ACS Chemical Neuroscience
Neil C Lax, Stacy-Ann J Parker, Edward J Hilton, Youstina Seliman, Kevin J Tidgewell, Benedict J Kolber
Marine cyanobacteria represent a unique source in the field of drug discovery due to the secondary metabolites they produce and the structural similarity these compounds have to endogenous mammalian receptor ligands. A series of cyanobacteria were subjected to extraction, fractionation by column chromatography and screened for affinity against CNS targets with a focus on serotonin receptors (5-HTRs). Out of 276 fractions screened, 21% had activity at 5-HTRs and/or the 5-HT transporter (SERT). One sample, a cyanobacterium identified by 16S rRNA sequencing as Leptolyngbya from Las Perlas archipelago in Panama, contained a fraction with noted affinity for the 5-HT7 receptor (5-HT7 R)...
July 10, 2018: Synapse
Cheng Xue Du, Yuan Guo, Qiao Jun Zhang, Jin Zhang, Shu Xuan Lv, Jian Liu
OBJECTIVE: At present, little is known about the role of serotonin7 (5-HT7 ) receptor in anxiety, particularly in Parkinson's disease-related anxiety. Here, we tested whether 5-HT7 receptors in the prelimbic (PrL) cortex are involved in the regulation of anxiety-like behaviors in sham-operated rats and rats with unilateral 6-hydroxydopamine lesions of the medial forebrain bundle (MFB). METHODS: The open field and elevated plus maze (EPM) tests were performed to study the influence of MFB lesion and intra-PrL injection of 5-HT7 agonist AS19 (0...
October 2018: Neurological Research
Ilhan Elmaci, Meric A Altinoz
Pimozide is currently being used in clinic as a neuroleptic and exerts versatile biological actions. Pimozide is a cationic amphiphilic drug (CAD); CADs block the synthesis of neutral lipids, impair cholesterol homeostasis of cancer cells and increase accumulation of diacylglycerol-3-phosphate. Pimozide exerts tumoricidal activity which was first shown for melanoma and neuroblastoma via proposed anti- dopaminergic effects. Recently, pancreas cancers are shown to elevate dopamine receptor-2 synthesis, which is blocked by pimozide leading growth inhibition...
August 2018: Critical Reviews in Oncology/hematology
Ádám Andor Kelemen, Grzegorz Satała, Andrzej J Bojarski, György M Keserű
Here we report the design and synthesis of spiro[pyrrolidine-3,3'-oxindole] derivatives representing a novel scaffold of 5-HT7 receptor ligands. The synthesized analogues were validated as low nanomolar ligands showing selectivity in a panel of related serotonin receptor subtypes including 5-HT1A R, 5-HT2A R and 5-HT6 R.
August 1, 2018: Bioorganic & Medicinal Chemistry Letters
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