Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P46098 (5-HT3 receptor)
 2,290 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effects of eight serotonin (5-HT) receptor antagonists on the anorectic effect of d-fenfluramine (3.0 mg/kg, IP) were examined in a test of sweet mash consumption, using non-deprived male rats. d-Fenfluramine's effect was attenuated by the mixed 5-HT1/5-HT2 receptor antagonists, methiothepin and metergoline; by the 5-HT2 receptor antagonist ritanserin; and by (+/-)cyanopindolol, a mixed 5-HT1A/5-HT1B receptor antagonist. In contrast, d-fenfluramine's effect was not antagonised by the 5-HT2 receptor antagonists ketanserin and ICI 169 369; the 5-HT3 receptor antagonist ICS 205 930; or by xylamidine, a peripheral 5-HT receptor antagonist. In this feeding model, none of the 5-HT antagonists, when tested alone, had any effect to increase palatable food consumption. The pattern of results obtained strongly suggest that central 5-HT1 receptors play an important role in the mediation of d-fenfluramine-induced anorexia.
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PMID:Evidence that d-fenfluramine anorexia is mediated by 5-HT1 receptors. 249 30

Previous behavioural studies have shown that 5-hydroxytryptamine3 (5-HT3) receptor antagonists either block or have no effect on amphetamine-induced effects. The present experiments investigated whether or not the highly selective 5-HT3 receptor antagonist ondansetron would affect the anorectic effect of a small dose (1 mg/kg) of d-amphetamine. Nondeprived male rats were tested in two feeding paradigms: consumption of a palatable sweetened mash and ingestion of a 3% sucrose solution. Ondansetron (10-100 micrograms/kg) did not antagonize amphetamine-induced anorexia; instead, in both paradigms consumption was reduced still further when the 5-HT3 antagonist was given in conjunction with amphetamine. Ondansetron given alone had significant effects on consumption, but the direction of the effect differed according to the paradigm. Sweetened mash intake was significantly increased at 30 and 100 micrograms/kg, while sucrose ingestion was significantly reduced at 10 and 30 micrograms/kg ondansetron. It is suggested that ondansetron has two opposing effects on intake, one of which (hyperphagia) can be masked by d-amphetamine, leaving an anorectic effect that augments that of d-amphetamine.
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PMID:The selective 5-HT3 receptor antagonist, ondansetron, augments the anorectic effect of d-amphetamine in nondeprived rats. 833 20

The efficacy of tropisetron, a new 5-HT3 receptor antagonist, was evaluated in a group of 15 children with a variety of malignant tumours. The majority of children (14/15) received fractionated chemotherapy and on day one complete control of acute nausea and vomiting was observed in 68.7% of all patients with a single, 15-minute, i.v. infusion of tropisetron. Partial control of vomiting was observed in 25% of patients and of nausea in 31.3% of patients on Day 1. Complete control of delayed nausea and vomiting was more variable, with an observed range between 50%-81% of patients over Days 2-6. There was no loss of appetite in 75% of patients treated with tropisetron on Day 1 and, more variably, in 62%-87% of patients on Days 2-6. Side effects were recorded in 18.8% of chemotherapy cycles, the most significant being insomnia in 12.5% of cycles and slight fever in 6.3% of cycles. It was concluded that tropisetron was well suited for children and could be recommended for those receiving a high burden of fractionated chemotherapy.
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PMID:Tropisetron in the control of nausea and vomiting induced by combined cancer chemotherapy in children. 836 98

Recently, granisetron (KYT), one of the 5-HT3 receptor antagonists, has been developed and proved to have a strong effect for cisplatin (CDDP)-induced emesis. The combination chemotherapy with CDDP and 5-fluorouracil (5-FU), which has great efficacy for head and neck cancer, induces nausea and vomiting as side effects. We compared the effects of KYT for CDDP plus 5-FU-induced emesis between two administration schedules. Forty patients were randomized to two groups. KYT was administered either on day 1 for twenty patients (Group A), or for consecutive 5 days in another twenty patients (Group B). Additional antiemetics were administered in thirteen patients in Group A and seven patients in Group B for severe nausea and vomiting even after KYT administration. The times of additional antiemetics administration were more frequent in Group B. The nausea score was statistically lower in Group B and the duration of nausea or vomiting was statistically longer in Group A. The frequency of vomiting was the same in the two groups on day 1, but it was controlled faster in Group B. Appetite loss was lower on day 7 in Group B. It was concluded that vomit and nausea were controlled better in Group B after day 4. Additional antiemetics were not effective, and 5 consecutive administrations of KYT for chemotherapy with CDDP plus 5-FU was effective for late emesis.
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PMID:[Comparison of effects between single vs five-day injection of granisetron for combination chemotherapy with cisplatin and 5-fluorouracil for head and neck cancer]. 923 62

Serotonin3 (5-HT3) receptors in the periphery mediate anorectic responses to the amino acid deficiency, which occurs after eating amino acid-imbalanced diets (IMB). However, other neurochemical systems, notably cholecystokinin (CCK), are known to affect food intake. We pretreated rats systemically with tropisetron, a 5-HT3 receptor antagonist, alone and combined with antagonists of CCK(A) and CCK(B) receptors, and measured intake of an IMB. Devazepide, a CCK(A) receptor antagonist, appeared to interact with tropisetron in the anorectic responses to IMB, blunting the usual remediation of IMB anorexia by tropisetron. The CCK(B) receptor antagonist, L-365, 260, increased intake of both IMB and an amino acid-balanced basal diet (BAS) and did not interact with tropisetron. Our data suggest that activation of CCK(A) receptors is interactive with 5-HT3 receptor activity in mediating IMB anorexia in the aminoprivic feeding model.
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PMID:CCK(A) and 5-HT3 receptors interact in anorectic responses to amino acid deficiency. 1008 Feb 41

The serotonin3 (5-HT3) receptor plays an important role in the aminoprivic feeding model. Other neurochemical systems, including cholecystokinin (CCK) and dopamine (DA), are known to affect food intake. We pretreated rats systemically with tropisetron, a 5-HT3 receptor antagonist, alone and combined with antagonists of DA1 and DA2 receptors, and measured intake of an amino acid-imbalanced diet (IMB). As expected, tropisetron significantly increased intake of IMB. SCH-23390, a DA1 antagonist, increased IMB anorexia. When combined with tropisetron, DA2 antagonism with eticlopride reduced short-term intake of both the basal diet (BAS) and IMB. In the IMB model, specificity of 5-HT3-DA2 interactions, and of 5-HT3-CCK(A) interactions from previous studies, prompted investigation of CCK(A)-DA2 interactions; there appeared to be none. SKF-38393, a DA1 agonist, combined with the CCK(A) receptor antagonist, devazepide, increased BAS and tended to increase IMB intake. Thus, CCK(A)-DA1 interactions were not specific for IMB. These data suggest that DA1 receptor activity opposes IMB anorexia, possibly via an interaction with the 5-HT3 receptor.
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PMID:DA1 receptor activity opposes anorectic responses to amino acid-imbalanced diets. 1008 Feb 42

The objective of this study was to evaluate the efficacy and safety of ramosetron hydrochloride for the management of nausea and vomiting induced by chemotherapy in patients with hematological malignancies. A total of 30 patients with hematological malignancies were included in the ramosetron group. Ramosetron (0.3 mg i.v.) was administered 0.5 h before chemotherapy. The impact of ramosetron on anorexia, nausea and vomiting as well as other adverse effects were assessed. Meanwhile, another 39 patients received tropisetron (o.d. for 3 days). As compared to the tropisetron group, the response rate of the ramosetron group in controlling anorexia within 18-24 h after chemotherapy was higher (p < 0.05); within 18-24 h after chemotherapy, the complete response rate and effective rate in controlling nausea was higher (p < 0.05); within 12-18 h and 18-24 h after chemotherapy, the complete response rate and effective rate in controlling vomiting was higher (p < 0.05). The incidence of adverse effects was similar in both groups. We conclude that ramosetron belongs to a new generation of 5-HT3 receptor antagonists and that it is a safe, economic and effective antiemetic drug.
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PMID:Ramosetron for the management of chemotherapy-induced gastrointestinal events in patients with hematological malignancies. 1167 27

This report outlines measures for controlling nausea, vomiting, and anorexia caused by anticancer agents. Combination therapy with a 5-hydroxytryptamine (5-HT3) receptor antagonist and a steroid preparation is effective for controlling acute vomiting. In the chronic stage, however, the response to 5-HT3 receptor antagonists is less marked, so a steroid preparation is used as the major treatment in combination with a 5-HT3-receptor antagonist or metoclopramide. The antiemetic effect of recently developed tachykinin NK-1 (NK-1)-receptor antagonists has been shown to be additive to that of existing treatments for acute and chronic symptoms, especially chronic nausea/vomiting. Steroid preparations have been shown to improve anorexia, while medroxyprogesterone acetate (MPA: a synthetic progesterone) has been reported to improve anorexia and promote weight gain.
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PMID:[Management of nausea, vomiting and anorexia due to anticancer agents]. 1285 41

Effective antiemetic therapy is crucial for patients undergoing chemotherapy or radiotherapy for cancer. Severe nausea and vomiting associated with such cancer treatment can lead to anxiety, anorexia, dehydration, electrolyte disturbance and renal failure, and may interrupt cancer therapy, demoralise patients or even cause them to abandon treatment. In 1992, we welcomed the introduction of ondansetron, the first selective serotonin type 3- (5HT3-) receptor antagonist marketed in the UK, as an important advance in preventing chemotherapy-induced nausea and vomiting. Several selective 5HT3-receptor antagonists are now licensed. They are widely prescribed to patients receiving cancer treatment, but not always appropriately. Here we review their optimal use.
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PMID:5HT3-receptor antagonists as antiemetics in cancer. 1611 Oct 85

We performed a retrospective study to examine the protective effect of low-dose dexamethasone (DEX) on delayed adverse events induced by carboplatin (CBDCA)-based combination chemotherapy in patients with thoracic tumors. Low-dose DEX (4-8 mg/day) was administered on day 1 and after, in addition to a serotonin 5-HT3 receptor antagonist. The acute adverse events (day 1) were well controlled in the patients with or without co-treatment of DEX. On the other hand, the delayed nausea, emesis, anorexia, and fatigue after day 2 failed to be controlled by 5-HT3 antagonist alone. Co-treatment with DEX significantly suppressed the grade of the delayed adverse events during days 2-10. The mean ratio of complete protection during days 2-10 were significantly higher in the DEX-treated group compared with the non-DEX-treated group. These results reveal that low-dose DEX is a clinically effective treatment for the prevention of delayed adverse events induced by CBDCA-based combination chemotherapy.
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PMID:Preventive effects of low-dose dexamethasone for delayed adverse events induced by carboplatin-based combination chemotherapy. 1754 Dec 51


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