Last update 01 Nov 2024

5-HT3 receptor x M3 receptor

Last update 01 Nov 2024

Basic Info

Related Targets

5-HT3 receptorM3 receptor

Drugs associated with 5-HT3 receptor x M3 receptor

Revatropate

Target

5-HT3 receptor x M3 receptor

Mechanism

5-HT3 receptor antagonists [+1]

Active Org.-

Originator Org.

Pfizer Inc.

Active Indication-

Inactive Indication

Pulmonary Disease, Chronic Obstructive

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with 5-HT3 receptor x M3 receptor

100 Translational Medicine associated with 5-HT3 receptor x M3 receptor

0 Patents (Medical) associated with 5-HT3 receptor x M3 receptor

Literatures (Medical) associated with 5-HT3 receptor x M3 receptor

01 Feb 2020·Anaesthesia Critical Care & Pain MedicineQ3 · MEDICINE

Genetic contribution to PONV risk

Q3 · MEDICINE

Article

Author: Hagen S. Bachmann ; Nina Seyffert ; Ulrich H. Frey ; Gudrun J. de Vries ; Laura Schiefer ; Jürgen Peters ; Stefanie Klenke

BACKGROUNDClinical risk factors for postoperative nausea and vomiting (PONV) are usually stratified using the Apfel Score. While a genetic predisposition has recently been demonstrated with the muscarinic acetylcholine receptor (CHRM3) rs2165870 single nucleotide polymorphism (SNP), we investigated whether (1) other SNPs contribute to PONV risk and (2) a genetic risk score might summarise genetic PONV risk.METHODSWe retrospectively analysed data from a study with 472 patients undergoing elective surgery. We investigated the SNPs rs3218315 (IL2RB), rs349358 (KCNB2), rs703363 (intergenic variant), rs1800497 (DRD2), rs1799971 (OPRM1), and rs1176713 (HTR3A). A genetic risk score was established and association with PONV investigated.RESULTSEarly PONV occurred in 37%. There was a significant association of the KCNB2 rs349358 SNP with nausea (P = 0.021), retching (P = 0.001), and PONV (P = 0.006). The rs349358 genotype distribution was TT in 310 and TC/CC in 155 patients. The KCNB2 SNP was associated with an Odds Ratio (OR) of 1.6 for CT/CC vs. TT (95% CI 1-2.5; P = 0.031) to develop PONV and this was independent from the Apfel Score, and the CHRM3 rs2165870 SNP. A genetic risk score based on the CHRM3 rs2165870 and the KCNB2 rs349358 SNP was created and this genetic score (OR per genetic risk score point: 1.6 (1.3-2.1), P < 0.0001) was independent from the Apfel Score (OR per Apfel score point: 1.6 (1.3-1.9), P < 0.0001) associated with PONV.CONCLUSIONThe KCNB2 rs349358 SNP is also an independent PONV predictor and a genetic risk score has a similar impact on PONV susceptibility compared to the Apfel Score.

25 Apr 2019·Zhen ci yan jiu = Acupuncture research

[Comparison of effects of electroacupuncture at "Tianshu" (ST25) and "Dachangshu" (BL25) on intestinal sensitivity and expression of muscarinic M₃R and 5-HT_3AR in irritable bowel syndrome rats].

Article

Author: Lan, Ying ; Guo, Meng-Wei ; Wang, Yi-Fan ; Gao, Yu-Shan ; Ji, Mao-Xian ; Zhang, Hong-Lin ; Wang, Shan ; Ren, Xiao-Xuan ; Qin, Ying

OBJECTIVETo observe and compare the effect of electroacupuncture (EA) of "Tianshu" (ST25) and "Dachangshu" (BL25) on intestinal sensitivity and the expression of M₃ muscarinic acetylcholine receptor (M₃R) and 5-hydroxytryptamine 3A receptor (5-HT_3AR) in the colon tissue in irritable bowel syndrome (IBS) rats, so as to explore its mechanism underlying improvement of IBS.METHODSForty newborn Wistar rats were randomly divided into blank control, model, ST25 and BL25 groups (n＝10 rats per group). The IBS model was established by joint application of maternal separation, acetic acid enema plus colorectal distension from day 8 to 21 after birth. At the age of 9 weeks, EA (2 Hz/100 Hz, 0.1－0.3 mA) was applied to ST25 and BL25 for 20 min, once every other day for 5 times. The modified method was used to record the abdominal withdrawal reflex (AWR), so as to evaluate the visceral sensitivity by referring to the modified Al-Chaer's and colleagues' methods. The threshold (initial wave), the number and peak-peak value of contraction waves (AWR) within 90 s were recorded. The immunoactivity of M₃R and 5-HT_3AR in the colon tissue was detected by immunohistochemistry.RESULTSAfter modeling, the latency was obviously shortened, the number and peak-peak values of contraction waves of intestine were significantly increased, and the immunoactivity of M₃R and 5-HT_3AR was notably up-regulated in the model group compared with the blank control group (P<0.01). After the EA intervention, the latency was obviously prolonged, the peak-peak value in both ST25 and BL25 groups, and the number of contraction waves in the ST25 group were significantly decreased (P<0.01), and the expression levels of M₃ and 5-HT_3A R were considerably down-regulated in both ST25 and BL25 groups relevant to the model group (P<0.01). The therapeutic effects were significantly better in the ST25 group than in the BL25 group in prolonging the latency and reducing the contraction wave number, and in down-regulating the expression of colonic M₃R and 5-HT_3AR (P<0.05, P<0.01).CONCLUSIONEA at ST25 and BL25 can reduce the intestinal sensitivity in IBS rats, which is probably associated with its effects in down-regulating the expression of M₃R and 5-HT_3AR in the colon. The therapeutic effects of ST25 were obviously better than those of BL25 in suppressing intestinal sensitivity and expression of colonic M₃R and 5-HT_3AR.

01 Jun 2018·Journal of Clinical Psychopharmacology

Genetic Polymorphisms Associated With Constipation and Anticholinergic Symptoms in Patients Receiving Clozapine

Article

Author: Kampman, Olli ; Leinonen, Esa ; Seppaelae, Niko ; Solismaa, Anssi ; Mononen, Nina ; Viikki, Merja ; Lehtimaeki, Terho ; Lyytikaeinen, Leo-Pekka

AbstractBackgroundClozapine impairs gastrointestinal motility owing to its anticholinergic and antiserotonergic properties. This commonly leads to constipation and potentially to more severe complications such as bowel obstruction and ischemia. The aim of this study was to determine whether genetic variations in the genes encoding muscarinic and serotonergic receptors (CHRM2, CHRM3, HTR2, HTR3, HTR4, and HTR7) explain the variations in incidence of constipation and anticholinergic symptoms during clozapine treatment. Genes associated with opiate-induced constipation were also included in this analysis (TPH1, OPRM1, ABCB1, and COMT).ProceduresBlood samples from 176 clozapine-treated, Finnish, white patients with schizophrenia were genotyped. Constipation and anticholinergic symptoms were rated using the Liverpool University Neuroleptic Side Effect Rating Scale self-report questionnaire. In total, 192 single-nucleotide polymorphisms (SNPs) were detected and grouped to formulate a weighted genetic-risk score (GRS).ResultsNo significant associations between individual SNPs or GRSs and constipation or laxative use were observed. A GRS of 19 SNPs in CHRM2, CHRM3, HTR3C, HTR7, ABCB1, OPRM1, and TPH1 was associated with anticholinergic symptoms in a generalized linear univariate model, with body mass index, clozapine monotherapy, and GRS as explaining variables (permuted P = 0.014). Generalized linear univariate model analysis performed on the opiate-induced constipation–associated SNPs and a single CHRM3 SNP revealed an association between anticholinergic symptoms and a score of 8 SNPs (adjusted P = 0.038, permuted P = 0.002).ConclusionsTwo GRSs are able to predict the risk of anticholinergic symptoms in patients receiving clozapine and possibly an increased risk of gastrointestinal hypomotility.

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