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https://www.readbyqxmd.com/read/28626482/the-possible-mechanisms-of-analgesia-produced-by-microinjection-of-morphine-into-the-lateral-habenula-in-the-acute-model-of-trigeminal-pain-in-rats
#1
Emad Khalilzadeh, Gholamreza Vafaei Saiah
This study aimed to assess the effect of intra-habenular injection of morphine on acute trigeminal pain in rats. Also here, we examined the involvement of raphe nucleus opioid and 5HT3 receptors on the antinociceptive activity of intra habenular morphine to explore the possibility of existence of descending antinociceptive relay between the habenula and raphe nucleus. The numbers of eye wiping response elicited by applying a drop (40 μL) of NaCl (5 M) solution on the corneal surface were taken as an index of acute trigeminal nociception...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28623711/contribution-of-dopaminergic-and-noradrenergic-systems-in-the-antinociceptive-effect-of-%C3%AE-phenylalanyl-acetophenone
#2
Fernanda S S Sousa, Roberta G Anversa, Paloma T Birmann, Maurice N de Souza, Renata Balaguez, Diego Alves, Cristiane Luchese, Ethel A Wilhelm, Lucielli Savegnago
BACKGROUND: This study evaluated the antinociceptive action of α-(phenylalanyl) acetophenone (PSAP) in mice. METHODS: Evaluated whether the serotonergic, adrenergic and dopaminergic systems are involved in PSAP antinociceptive activity. PSAP was administered intragastrically (ig) 30min prior to formalin or glutamate test and compared with a standard drug, meloxicam (10mg/kg, ig). RESULTS: The treatment with PSAP (10-50mg/kg) caused inhibition in the neurogenic phase and reduced the paw oedema caused by intraplantar (ipl) injection of formalin...
March 27, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28616820/possible-involvement-of-central-oxytocin-in-cisplatin-induced-anorexia-in-rats
#3
Koichi Arase, Hirofumi Hashimoto, Satomi Sonoda, Hiromichi Ueno, Reiko Saito, Yasuhito Motojima, Mitsuhiro Yoshimura, Takashi Maruyama, Keiji Hirata, Yasuhito Uezono, Yoichi Ueta
During cancer chemotherapy, drugs such as 5-HT3 receptor antagonists have typically been used to control vomiting and anorexia. We examined the effects of oxytocin (OXT), which has been linked to appetite, on cisplatin-induced anorexia in rats. Fos-like immunoreactivity (Fos-LI) expressed in the supraoptic nucleus (SON), the paraventricular nucleus (PVN), the area postrema and the nucleus of the solitary tract (NTS) after intraperitoneal (ip) administration of cisplatin. We also examined the fluorescence intensity of OXT-mRFP1 after ip administration of cisplatin in OXT-mRFP1 transgenic rats...
June 14, 2017: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28612633/granisetron-in-the-treatment-of-chemotherapy-induced-nausea-and-vomiting-cinv-is-there-still-a-role-after-comparison-with-palonosetron
#4
Sheila A Doggrell
Chemotherapy-induced nausea and vomiting (CINV) has a negative impact on the lives of subjects receiving chemotherapy. In 2009, the second generation 5-HT3-receptor antagonist, palonosetron, which is longer-acting than granisetron, was shown, as part of dual therapy with dexamethasone, to be superior to intravenous granisetron in the delayed phase of CINV. Area covered: In an attempt to maintain plasma levels of granisetron during the delayed phase of CINV, longer-acting preparations of granisetron have been manufactured...
June 19, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28595448/do-patients-receiving-pelvic-radiation-and-anti-emetics-experience-diarrhea-and-or-constipation
#5
Leah Drost, Vithusha Ganesh, Bo Angela Wan, Carlo DeAngelis, Mark Pasetka, May Tsao, Elizabeth Barnes, Hans Chung, Edward Chow
BACKGROUND: Pelvic radiation may cause radiation enteritis, which commonly manifests as diarrhea. Radiation to the abdomen or pelvis may also cause radiation-induced nausea and vomiting (RINV) which is often treated with anti-emetics such as serotonin (5-HT3) receptor antagonists (RA). However, a common side effect of these anti-emetic medications is constipation. Both diarrhea and constipation can have a significant impact on patient quality of life (QOL). The objective of this study was to assess the prevalence of diarrhea and constipation in patients receiving pelvic radiation and anti-emetics...
June 3, 2017: Annals of Palliative Medicine
https://www.readbyqxmd.com/read/28550529/single-administration-of-hbk-15-a-triple-5-ht1a-5-ht7-and-5-ht3-receptor-antagonist-reverses-depressive-like-behaviors-in-mouse-model-of-depression-induced-by-corticosterone
#6
Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Anna Waszkielewicz, Agnieszka Kij, Maria Walczak
Studies suggest that the blockade of 5-HT1A, 5-HT7, and 5-HT3 receptor may increase the speed of antidepressant response. 1-[(2,6-Dimethylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15), dual 5-HT1A and 5-HT7 antagonists, showed significant antidepressant- and anxiolytic-like properties in our previous tests in rodents. In this study, we aimed to investigate their antidepressant potential using mouse model of corticosterone-induced depression...
May 26, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28535979/mirtazapine-fatal-poisoning
#7
Claudia Vignali, Angelo Groppi, Francesca Brandolini, Francesco Maria Avato, Anna Talarico, Rosa Maria Gaudio, Luca Morini
Mirtazapine is a noradrenergic and specific serotoninergic antidepressant agent that stimulates norepinephrine and serotonin release while also blocking serotonin receptors (5-HT2 and 5-HT3). Although the drug is used extensively, at present we do not know of any fatal cases due to mirtazapine alone. On the contrary, the published literature describes several fatal poisoning cases related to the intake of mirtazapine together with other drugs. Here we describe a fatal case of mirtazapine self-poisoning, since the other drug detected (lorazepam), was within the therapeutic range...
May 8, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28533557/the-developmental-emergence-of-differential-brainstem-serotonergic-control-of-the-sensory-spinal-cord
#8
F Schwaller, A H Kanellopoulos, M Fitzgerald
Descending connections from brainstem nuclei are known to exert powerful control of spinal nociception and pain behaviours in adult mammals. Here we present evidence that descending serotonergic fibres not only inhibit nociceptive activity, but also facilitate non-noxious tactile activity in the healthy adult rat spinal dorsal horn via activation of spinal 5-HT3 receptors (5-HT3Rs). We further show that this differential serotonergic control in the adult emerges from a non-modality selective system in young rats...
May 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526687/ffa2-activation-combined-with-ulcerogenic-cox-inhibition-induces-duodenal-mucosal-injury-via-the-5-ht-pathway-in-rats
#9
Yasutada Akiba, Koji Maruta, Kazuyuki Narimatsu, Hyder Said, Izumi Kaji, Ayaka Kuri, Ken-Ichi Iwamoto, Atsukazu Kuwahara, Jonathan D Kaunitz
Serotonin (5-HT), predominantly synthesized and released by enterochromaffin cells, is implicated in gastrointestinal symptoms such as emesis, abdominal pain and diarrhea. Since luminal short-chain fatty acids (SCFAs) release 5-HT from enterochromaffin cells, which express the SCFA receptor FFA2 in rat duodenum, we examined the effects of the selective FFA2 agonist phenylacetamide-1 (PA1) on duodenal 5-HT release with consequent bicarbonate secretion (DBS) and on indomethacin (IND)-induced enteropathy. Intestinal injury was induced by IND (10 mg/kg, sc) with or without PA1...
May 19, 2017: American Journal of Physiology. Gastrointestinal and Liver Physiology
https://www.readbyqxmd.com/read/28514235/ondansetron-does-not-reduce-withdrawal-in-patients-with-physical-dependence-on-chronic-opioid-therapy
#10
Larry F Chu, John Sun, Anna Clemenson, Matthew J Erlendson, Tom Rico, Erika Cornell, Hannah Obasi, Zahra N Sayyid, Ellen M Encisco, Jeff Yu, Jamison G Gamble, Ian Carroll, J David Clark
OBJECTIVES: Individuals taking opioids for an extended period of time may become physically dependent, and will therefore experience opioid withdrawal should they stop taking the medication. Previous work in animal and human models has shown that the serotonin (5-HT3) receptor may be implicated in opioid withdrawal. In this study, we investigated if ondansetron, a 5-HT3-receptor antagonist, could reduce the symptoms of opioid withdrawal after chronic opioid exposure in humans. METHODS: In this double-blinded, randomized, crossover study, 33 chronic back pain patients (N = 33) were titrated onto sustained-release oral morphine for 30 days...
May 16, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28501575/the-anti-asthmatic-drug-pranlukast-suppresses-the-delayed-phase-vomiting-and-reverses-intracellular-indices-of-emesis-evoked-by-cisplatin-in-the-least-shrew-cryptotis-parva
#11
Nissar A Darmani, Seetha Chebolu, Weixia Zhong, William D Kim, Matthew Narlesky, Joia Adams, Fanglong Dong
The introduction of second generation serotonin 5-HT3 receptor (5-HT3) antagonist palonosetron combined with long-acting substance P neurokinin NK1 receptor (NK1) antagonists (e.g. netupitant) has substantially improved antiemetic therapy against early- and delayed-phases of emesis caused by highly emetogenic chemotherapeutics such as cisplatin. However, the improved efficacy comes at a cost that many patients cannot afford. We introduce a new class of antiemetic, the antiasthmatic leukotriene CysLT1 receptor antagonist pranlukast for the suppression of cisplatin-evoked vomiting...
May 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28500750/nausea-and-vomiting-in-children-and-adolescents-receiving-intrathecal-methotrexate-a-prospective-observational-study
#12
Jacqueline Flank, Komail Nadeem, Sheliza Moledina, Mila Khanna, Christina Schindera, Angela Punnett, L Lee Dupuis
BACKGROUND: The prevalence of nausea and vomiting after receipt of intrathecal methotrexate (IT-MTX) in pediatric oncology patients is unknown. METHODS: Patients (4-18 years) about to receive IT-MTX were eligible to participate in this prospective, observational study. Patients received antiemetics as prescribed by their clinical team. Nausea severity (patient-assessed), timing of emetic episodes, and administration of antiemetics were recorded beginning immediately prior to IT-MTX administration, for the next 24 hr (acute phase), and for a maximum of 7 additional days (delayed phase)...
May 13, 2017: Pediatric Blood & Cancer
https://www.readbyqxmd.com/read/28499187/vortioxetine-a-review-of-the-pharmacology-and-clinical-profile-of-the-novel-antidepressant
#13
REVIEW
Magdalena Sowa-Kućma, Patrycja Pańczyszyn-Trzewik, Paulina Misztak, Rafał R Jaeschke, Katherine Sendek, Krzysztof Styczeń, Wojciech Datka, Magdalena Koperny
The aim of this paper was to review the up-to-date evidence base on pharmacology and clinical properties of vortioxetine. Vortioxetine is a novel antidepressant, approved by the US Food and Drug Administration (FDA) for the treatment of major depressive disorder (MDD). Because vortioxetine exhibits both an antidepressant and anxiolytic effect, it may be effective in treating both depressive and anxiety disorders, such as generalized anxiety disorder (GAD). Based on its pharmacodynamics profile and preclinical studies, it is believe that the drug's clinical action is mediated mainly by selective blockade of serotonin reuptake (by inhibiting the serotonin transporter [SERT]) and direct modulation of 5-HT receptors activity (such as 5-HT3, 5-HT7, 5-HT1D and 5-HT1B)...
February 1, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28496413/cholera-toxin-induces-sustained-hyperexcitability-in-myenteric-but-not-submucosal-ah-neurons-in-guinea-pig-jejunum
#14
Katerina Koussoulas, Rachel M Gwynne, Jaime P P Foong, Joel C Bornstein
Background and Aims: Cholera toxin (CT)-induced hypersecretion requires activation of secretomotor pathways in the enteric nervous system (ENS). AH neurons, which have been identified as a population of intrinsic sensory neurons (ISNs), are a source of excitatory input to the secretomotor pathways. We therefore examined effects of CT in the intestinal lumen on myenteric and submucosal AH neurons. Methods: Isolated segments of guinea pig jejunum were incubated for 90 min with saline plus CT (12.5 μg/ml) or CT + neurotransmitter antagonist, or CT + tetrodotoxin (TTX) in their lumen...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28493335/response-of-htr3a-ko-mice-to-antidepressant-treatment-and-chronic-stress
#15
Vincent Martin, Armance Riffaud, Tevrasamy Marday, Charly Brouillard, Bernard Franc, Jean-Pol Tassin, Caroline Sevoz-Couche, Raymond Mongeau, Laurence Lanfumey
BACKGROUND AND PURPOSE: It has recently been suggested that 5-HT3 receptor blockade enhances selective serotonin reuptake inhibitor (SSRI) antidepressants efficacy and may reverse stress-induced deficits in rodents. EXPERIMENTAL APPROACH: To further explore this hypothesis, we used mice lacking the 5-HT3 receptor (Htr3a KO) and their wild-type (WT) controls to assess their response in behavioural paradigms relevant to anxiety and depression. Mice were studied under basal, antidepressant treatments and chronic social defeat stress (CSDS) conditions...
May 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28493078/the-5-ht3-receptor-antagonist-ondansetron-attenuates-pancreatic-injury-in-cerulein-induced-acute-pancreatitis-model
#16
Atsushi Tsukamoto, Takuto Sugimoto, Yuta Onuki, Hajime Shinoda, Taiki Mihara, Masatoshi Hori, Tomo Inomata
The 5-hydroxytryptamine-3 receptor (5-HT3R) antagonist ondansetron has been clinically approved as an anti-emetic agent. Recent findings indicate that ondansetron has anti-inflammatory properties. The aim of the present study was to assess the therapeutic action of ondansetron in cerulein-induced acute pancreatitis model. Male-BALB/c mice were used in the present study. Acute pancreatitis was induced by an hourly injection of cerulein. Ondansetron was administered subcutaneously at a dose of 3 mg/kg. The messenger RNA (mRNA) expression of 5-HT3 R in pancreatic tissue was assessed with RT-PCR...
May 10, 2017: Inflammation
https://www.readbyqxmd.com/read/28486926/5-ht3-receptors-a-potential-therapeutic-target-for-epilepsy
#17
Hongyan Zhao, Pu Wang, Shurui Chen, Xin Li, Hongliang Huo
Epilepsy is a syndrome of brain dysfunction caused by spontaneous, abnormal discharge. Many anti-epileptic drugs have developed in past decades. 5-HT is an important neurotransmitter in the central and peripheral nervous system of the human body which is involved in a number of physiological activities, such as sensation, movement, and behavior. 5-HT subtype have been divided into seven sub-groups from 5-HT1 to 5HT7. An increasing number of studies have shown that the activation of the 5-HT3 receptor can inhibit epileptic seizures, while inhibition of the 5HT3 receptor can promote spike waves...
May 8, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28453189/guideline-for-the-prevention-of-acute-chemotherapy-induced-nausea-and-vomiting-in-pediatric-cancer-patients-a-focused-update
#18
Priya Patel, Paula D Robinson, Jennifer Thackray, Jacqueline Flank, Mark T Holdsworth, Paul Gibson, Andrea Orsey, Carol Portwine, Jason Freedman, Jennifer R Madden, Robert Phillips, Lillian Sung, L Lee Dupuis
This update of the 2013 clinical practice guideline provides clinicians with guidance regarding the use of aprepitant and palonosetron for the prevention of acute chemotherapy-induced nausea and vomiting (CINV) in children. The recommendations were based on three systematic reviews. Substantive changes were made to the guideline recommendations including the inclusion of palonosetron to the 5-HT3 antagonists recommended for children receiving highly emetogenic chemotherapy (HEC) and the recommendation of aprepitant for children 6 months of age or older receiving HEC...
April 28, 2017: Pediatric Blood & Cancer
https://www.readbyqxmd.com/read/28447301/management-of-chemotherapy-induced-nausea-and-vomiting-in-pediatric-patients
#19
REVIEW
Rudolph M Navari
Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life and is perceived by patients as a major adverse effect of the treatment. This review summarizes the safety and efficacy of current antiemetic agents for the prevention of CINV in children. Information on antiemetic prophylaxis for CINV in children was obtained from a literature review of current peer-reviewed articles and recent international guidelines. The literature review and the international antiemetic guidelines provide recommendations for use of specific antiemetics in children based on the emetogenicity of the chemotherapy...
June 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/28439683/genistein-modulation-of-seizure-involvement-of-estrogen-and-serotonin-receptors
#20
Saeed Amiri Gheshlaghi, Razieh Mohammad Jafari, Mohammad Algazo, Nastaran Rahimi, Hussein Alshaib, Ahmad Reza Dehpour
Genistein, a major source of phytoestrogen exposure for humans and animals, has been shown to mediate neuroprotection in Alzheimer's disease and status epilepticus. In the present study, we investigated the effect of genistein on pentylenetetrazole-induced seizures in ovariectomized mice and the possible involvement of estrogenic and serotonergic pathways in the probable effects of genistein. Intraperitoneal (i.p.) administration of genistein (10 mg/kg) significantly increased the seizure threshold 30 min prior to induction of seizures 14 days after ovariectomy surgery...
July 2017: Journal of Natural Medicines
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