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María Rodríguez-Muñoz, Pilar Sánchez-Blázquez, Javier Garzón
Fenfluramine exhibits antiepileptic properties and thus diminishes epileptiform discharges in experimental animal models of Dravet syndrome. Fenfluramine is metabolized into norfenfluramine in vivo , which shows greater affinity and agonist activity at serotonin 5HT2 receptors (5HT2R) than fenfluramine. In this study, we found that fenfluramine and norfenfluramine disrupted the regulatory association of the sigma 1 receptor (σ1R) with NR1 subunits of glutamate N -methyl-D-aspartate receptors (NMDAR), an effect that was also produced by σ1R antagonists such as S1RA and prevented by σ1R agonists such as PPCC...
May 4, 2018: Oncotarget
Ibis M Agosto, Nicole L Nichols, Gordon S Mitchell
Although systemic inflammation induced by even a low dose of lipopolysaccharide (LPS, 100uL/kg) impairs respiratory motor plasticity, little is known concerning cellular mechanisms giving rise to this inhibition. Phrenic motor facilitation (pMF) is a form of respiratory motor plasticity elicited by pharmacological agents applied to the cervical spinal cord, or by acute intermittent hypoxia (AIH; 3, 5 min hypoxic episodes); when elicited by AIH, pMF is known as phrenic long-term facilitation (pLTF). AIH consisting of moderate hypoxic episodes (mAIH, PaO2 = 35-55 mmHg) elicits pLTF via the Q- pathway to pMF, a mechanism that requires spinal serotonin (5HT2) receptor activation and new BDNF protein synthesis...
March 7, 2018: Journal of Neurophysiology
Chrislean Jun Botanas, June Bryan de la Peña, Raly James Custodio, Irene Joy Dela Peña, Mikyung Kim, Taeseon Woo, Hee Jin Kim, Hye In Kim, Min Chang Cho, Yong Sup Lee, Jae Hoon Cheong
Depression afflicts around 16% of the world's population, making it one of the leading causes of disease burden worldwide. Despite a number of antidepressants available today, the delayed onset time and low remission rate of these treatments are still a major challenge. The N-methyl-D-aspartate (NMDA) receptor antagonist ketamine has shown to produce rapid and sustained antidepressant effects and has paved the way for a new generation of glutamate-based antidepressants. Methoxetamine (MXE) is a ketamine analogue that acts as an NMDA receptor antagonist and a serotonin reuptake inhibitor...
November 2017: Neuropharmacology
Jaeseong Oh, SeungHwan Lee, Anhye Kim, Jangsoo Yoon, Kyungho Jang, Doo H Lee, Sunyoung Cho, Sang Rim Lee, Kyung-Sang Yu, Jae-Yong Chung
VVZ-149, a dual antagonist of GlyT2 and 5HT2 A receptors, is an investigational analgesic with a novel mechanism of action that is currently under early-stage clinical development as an injectable agent for the treatment of postoperative pain. Here, the safety, tolerability, and pharmacokinetics of VVZ-149 injections in healthy male volunteers were explored in a randomized, double-blind, single- and multiple-ascending-dose (SAD and MAD, respectively), placebo-controlled clinical study. Subjects randomly received a 4-hour intravenous infusion of 0...
August 16, 2017: Journal of Clinical Pharmacology
S Mornese Pinna, E Scarvaglieri, M G Milia, D Imperiale, V Ghisetti, S Audagnotto, A Prochet, F Lipani, S Bonora, G Di Perri, A Calcagno
In the absence of effective prophylaxis and treatment, therapeutic options in HIV-positive patients with progressive multifocal leukoencephalopathy (PML) are limited to antiretroviral therapy: nevertheless, outcome is poor. We conducted a retrospective study (2009-2015) describing the outcome of 25 HIV-positive patients with detectable cerebrospinal fluid JC virus DNA: 14 had a probable PML while the others had evidence of other inflammatory central nervous system (CNS) affecting disorders. In the former group, 6-month mortality was 45...
October 2017: Journal of Neurovirology
Chihiro Shiratori, Nanoka Suzuki, Yuto Momohara, Kyosuke Shiraishi, Hitoshi Aonuma, Toshiki Nagayama
Phototactic behaviours are observed from prokaryotes to amphibians and are a basic form of orientation. We showed that the marbled crayfish displays phototaxis in which the behavioural response reversed from negative to positive depending on external light conditions. Animals reared in a 12-L/12-D light cycle showed negative phototaxis during daytime and positive phototaxis during night-time. Animals reared under constant light conditioning showed negative phototaxis during day- and night-time, while animals reared under constant dark conditioning showed positive phototaxis during day- and night-time...
August 2017: European Journal of Neuroscience
Tsuyoshi Hattori, Philippe Lluel, Céline Rouget, Moèz Rekik, Mitsuharu Yoshiyama
PURPOSE: The aim of this study was to assess the potential involvement of a specific subtype of 5-hydroxytryptamine (5-HT), 5HT2 receptors in neurally-induced contractions of the human detrusor. METHODS: Contractile responses to electrical field stimulation (EFS) were examined in human isolated urinary bladder muscle strips. The potentiation of EFS-induced detrusor contraction was examined by adding cumulative concentrations of a 5-HT and 5-HT2 receptor agonist, α-methyl-serotonin (α-Me-5-HT) (1nM-100μM) in the presence or absence of a 5-HT2 antagonist, ketanserin (5-HT2A>5-HT2C) or naftopidil (5-HT2B>5-HT2A) (0...
March 24, 2017: International Neurourology Journal
Masakatsu Fujinoki, Gen L Takei
Sperm hyperactivation is regulated by hormones present in the oviduct. In hamsters, 5-hydroxytryptamine (5HT) enhances hyperactivation associated with the 5HT2 receptor and 5HT4 receptor, while 17β-estradiol (E2) and γ-aminobutyric acid (GABA) suppress the association of the estrogen receptor and GABAA receptor, respectively. In the present study, we examined the regulatory interactions among 5HT, GABA, and E2 in the regulation of hamster sperm hyperactivation. When sperm were exposed to E2 prior to 5HT exposure, E2 did not affect 5HT-enhanced hyperactivation...
February 16, 2017: Journal of Reproduction and Development
Luisa Ponzoni, Daniela Braida, Mariaelvina Sala
No abstract text is available yet for this article.
December 2016: Psychopharmacology
S A Onasanwo, S O Faborode, K O Ilenre
Buchholzia coriacea, taken by elderly, has phytochemicals that have neuro-active metabolites, and the folkloredocumented its use in neuro-behavioral despairs. Previous study in our laboratory shows that methanol extracts of Buchholziacoriacea (MEBC) seeds possess antidepressant-like potentials in laboratory rodents. This present study was conducted toinvestigate the probable mechanism(s) of action by which MEBC potentiates its effects using laboratory rodents.Involvements of serotonergic, cholinergic and adrenergic systems were studied using Forced Swimming Test (FST) and TailSuspension Test (TST) models of behavioral despair...
August 30, 2016: Nigerian Journal of Physiological Sciences: Official Publication of the Physiological Society of Nigeria
Isabella Salzer, Enkhbileg Gantumur, Arsalan Yousuf, Stefan Boehm
Serotonin (5HT) is a constituent of the so-called "inflammatory soup" that sensitizes nociceptors during inflammation. Nevertheless, receptors and signaling mechanisms that mediate an excitation of dorsal root ganglion (DRG) neurons by 5HT remained controversial. Therefore, capsaicin-sensitive nociceptive neurons dissociated from rat DRGs were used to investigate effects of 5HT on membrane excitability and currents through ligand- as well as voltage-gated ion channels. In 58% of the neurons tested, 5HT increased action potential firing, an effect that was abolished by the 5HT2 receptor antagonist ritanserin, but not by the 5HT3 antagonist tropisetron...
November 2016: Neuropharmacology
Luisa Ponzoni, Daniela Braida, Mariaelvina Sala
RATIONALE: The synthetic phenethylamines are recreational drugs known to produce psychostimulant effects. However, their abuse potential has not been widely studied. OBJECTIVES: Here, we investigated the rewarding and the hallucinatory effects of 2,5-dimetoxy-4-bromo-amphetamine hydrobromide (DOB) and para-methoxyamphetamine (PMA) in comparison with the classical 3,4-methylenedioxymethamphetamine (MDMA). In addition, the role of serotonin 5-HT2-like receptor on the abovementioned effects was evaluated...
August 2016: Psychopharmacology
Bruna Balbino de Paula, Christie Ramos Andrade Leite-Panissi
The tonic immobility (TI) response is an innate fear behavior associated with intensely dangerous situations, exhibited by many species of invertebrate and vertebrate animals. In humans, it is possible that TI predicts the severity of posttraumatic stress disorder symptoms. This behavioral response is initiated and sustained by the stimulation of various groups of neurons distributed in the telencephalon, diencephalon and brainstem. Previous research has found the highest Fos-IR in the posteroventral part of the medial nucleus of the amygdala (MEA) during TI behavior; however, the neurotransmission of this amygdaloid region involved in the modulation of this innate fear behavior still needs to be clarified...
July 15, 2016: Brain Research
Miklós Palotai, Gyula Telegdy, Zsolt Bagosi, Miklós Jászberényi
Neuropeptide AF (NPAF) is an amidated octadecapeptide, which is member of the RFamide peptide family. NPAF is encoded by the farp-1 gene and acts through the G protein coupled NPFF-1 and NPFF-2 receptors. NPAF is involved in several physiological functions of the central nervous system, however we have little evidence about the involvement of NPAF in learning and memory. Therefore, the aim of the present study was to investigate the action of NPAF on consolidation of memory in a passive avoidance learning paradigm in mice...
January 2016: Neurobiology of Learning and Memory
Shawn P Alter, Kristen A Stout, Kelly M Lohr, Tonya N Taylor, Kennie R Shepherd, Minzheng Wang, Thomas S Guillot, Gary W Miller
We previously demonstrated that mice with reduced expression of the vesicular monoamine transporter 2 (VMAT2 LO) undergo age-related degeneration of the catecholamine-producing neurons of the substantia nigra pars compacta and locus ceruleus and exhibit motor disturbances and depressive-like behavior. In this work, we investigated the effects of reduced vesicular transport on the function and viability of serotonin neurons in these mice. Adult (4-6 months of age), VMAT2 LO mice exhibit dramatically reduced (90%) serotonin release capacity, as measured by fast scan cyclic voltammetry...
January 2016: Experimental Neurology
Joana Sotto Mayor, Ana Paula Pacheco, Sofia Esperança, Antonio Oliveira e Silva
Trazodone is a second-generation atypical antidepressant exercising selective inhibitory action on the transport of serotonin. It also has an antagonist effect, similar to nefazodone, on the 5HT1 and 5HT2 receptors, probably due to the therapeutic effects of such substances. It is very effective in the treatment of depression, in anxiety and insomnia. Its known side effects mainly occur with prolonged use of daily doses of 150-200 mg. The ability to enhance drowsiness may be associated with some risk in elderly patients...
July 14, 2015: BMJ Case Reports
Mohammad Abdollahi, Mansoureh Toghae, Firoozeh Raisi, Elaheh Saffari
BACKGROUND: Female sexual dysfunction (FSD) defines as any disorder in the process of sexual contact including 6 main domains, desire, arousal, lubrication, orgasm, orgasm satisfaction and pain. This study was conducted to evaluate prevalence of sexual dysfunction disorder in women with migraine headache and also find the associated factors related to migraine characteristics. METHODS: A total of 69 eligible woman patients fulfilling criteria for migraine participated in this study...
January 5, 2015: Iranian Journal of Neurology
G Telegdy, A Adamik
The action of PACAP-38 was studied by measuring the anxiogenic-anxiolytic behavior of rats in an elevated plus maze. PACAP-38 was administered into the lateral brain ventricle and the behavior of the animals was measured 3h later. The possible involvement of transmitters was measured by pretreating the animals with receptor blockers which alone did not influence the task, but in the doses used were effective with other neuropeptides. The receptor antagonist PACAP 6-38 (a PAC 1/VPAC2 receptor antagonist of PACAP-38 receptor), haloperidol (a non-selective dopamine receptor antagonist), phenoxybenzamine (an α1/α2β-adrenergic receptor antagonist), propranolol(a β-adrenergic receptor antagonist), bicuculline (a gamma-aminobutyric acid subunit A receptor antagonist), methysergide (a nonselective 5-HT2 serotonergic receptor antagonist), atropine (a nonselective muscarinic acetylcholine receptor antagonist), naloxone (a nonselective opioid receptor antagonist) and nitro-l-arginine which acts by blocking the enzyme nitric oxide synthase, thereby blocking the nitric oxide synthesis, were tested...
March 15, 2015: Behavioural Brain Research
Miklós Palotai, Gyula Telegdy, Masaru Tanaka, Zsolt Bagosi, Miklós Jászberényi
Little is known about the action of neuropeptide AF (NPAF) on anxiety and depression. Only our previous study provides evidence that NPAF induces anxiety-like behavior in rats. Therefore, the aim of the present study was to investigate the action of NPAF on depression-like behavior and the underlying neurotransmissions in mice. In order to determine whether there are species differences between rats and mice, we have investigated the action of NPAF on anxiety-like behavior in mice as well. A modified forced swimming test (mFST) and an elevated plus maze test (EPMT) were used to investigate the depression and anxiety-related behaviors, respectively...
November 1, 2014: Behavioural Brain Research
L Ratna, S Mukergee
Studies estimate that 1 in 6 women and 1 in 10 men experience childhood sexual abuse (CSA). Whilst ill-health is not an inevitable consequence, approximately 20% of victims go on to have serious long-term pathology. This is reflected in an excess incidence of CSA survivors in problem populations, be they medical, forensic or psychiatric. Four groups of research studies suggest that PTSD-related mechanisms might be a major mediating factor in the development of symptoms: 1. There is high incidence of PTSD following sexual trauma; 2...
1998: International Journal of Psychiatry in Clinical Practice
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