FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2806767306> ?p ?o ?g. }

• W2806767306 endingPage "331" @default.
• W2806767306 startingPage "322" @default.
• W2806767306 abstract "Stress urinary incontinence (SUI) is characterized by involuntary leakage associated with exertion, effort, sneezing, coughing, or lifting. Duloxetine, a serotonin norepinephrine reuptake inhibitor, is approved for the treatment of patients with SUI in some European countries, but not in the United States. There is currently no globally approved pharmacological drug for the treatment of patients with SUI. Therefore, a new pharmacological treatment option is required. TAS-303 [4-piperidinyl 2,2-diphenyl-2-(propoxy-1,1,2,2,3,3,3-day7 )acetate hydrochloride] is a novel small-molecule selective norepinephrine reuptake inhibitor that displays significant norepinephrine transporter (NET) inhibitory activity toward the serotonin or dopamine transporters. In this report, we describe the pharmacological properties of TAS-303 and its effects on urethral function, using preclinical in vitro and in vivo studies. Radioligand-binding studies showed that TAS-303 selectively and potently inhibited [3H]norepinephrine binding to the human NET. Oral administration of TAS-303 (3 mg/kg) significantly increased norepinephrine levels in the plasma, whereas it did not significantly affect epinephrine, dopamine, and serotonin levels. TAS-303 (0.3, 1, and 3 mg/kg) dose-dependently increased basal urethral pressure in normal rats and leak point pressure in vaginal distention rats, exhibiting a maximal effect comparable to duloxetine. In the forced swimming test, TAS-303 (100 mg/kg) showed no significant effects on immobility time in rats, raising the possibility that this agent would have minimal central nervous system side effects at an effective dose for urethral function. These results demonstrate that TAS-303 has therapeutic potential for the treatment of patients with SUI." @default.
• W2806767306 created "2018-06-13" @default.
• W2806767306 creator A5025830431 @default.
• W2806767306 creator A5047255008 @default.
• W2806767306 creator A5057859275 @default.
• W2806767306 creator A5083043049 @default.
• W2806767306 date "2018-06-06" @default.
• W2806767306 modified "2023-09-24" @default.
• W2806767306 title "TAS-303, a Novel Selective Norepinephrine Reuptake Inhibitor that Increases Urethral Pressure in Rats, Indicating Its Potential as a Therapeutic Agent for Stress Urinary Incontinence" @default.
• W2806767306 cites W1604629913 @default.
• W2806767306 cites W1966781628 @default.
• W2806767306 cites W1967312126 @default.
• W2806767306 cites W1970894908 @default.
• W2806767306 cites W1971918567 @default.
• W2806767306 cites W1972751776 @default.
• W2806767306 cites W1973386992 @default.
• W2806767306 cites W1974774230 @default.
• W2806767306 cites W1980067374 @default.
• W2806767306 cites W1986758727 @default.
• W2806767306 cites W1992269217 @default.
• W2806767306 cites W1994831553 @default.
• W2806767306 cites W1995496865 @default.
• W2806767306 cites W2010882816 @default.
• W2806767306 cites W2011713764 @default.
• W2806767306 cites W2017829997 @default.
• W2806767306 cites W2021316725 @default.
• W2806767306 cites W2037456922 @default.
• W2806767306 cites W2039382952 @default.
• W2806767306 cites W2058098475 @default.
• W2806767306 cites W2087789322 @default.
• W2806767306 cites W2092114190 @default.
• W2806767306 cites W2094380484 @default.
• W2806767306 cites W2106353554 @default.
• W2806767306 cites W2115562984 @default.
• W2806767306 cites W2124733814 @default.
• W2806767306 cites W2140598764 @default.
• W2806767306 cites W2143237569 @default.
• W2806767306 cites W2150242878 @default.
• W2806767306 cites W2156209231 @default.
• W2806767306 cites W2160327091 @default.
• W2806767306 cites W2167469143 @default.
• W2806767306 cites W2167880945 @default.
• W2806767306 cites W2170740534 @default.
• W2806767306 cites W2314756433 @default.
• W2806767306 cites W2441438395 @default.
• W2806767306 cites W2792472639 @default.
• W2806767306 cites W4236089062 @default.
• W2806767306 cites W60025275 @default.
• W2806767306 doi "https://doi.org/10.1124/jpet.118.248039" @default.
• W2806767306 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29875227" @default.
• W2806767306 hasPublicationYear "2018" @default.
• W2806767306 type Work @default.
• W2806767306 sameAs 2806767306 @default.
• W2806767306 citedByCount "10" @default.
• W2806767306 countsByYear W28067673062018 @default.
• W2806767306 countsByYear W28067673062019 @default.
• W2806767306 countsByYear W28067673062020 @default.
• W2806767306 countsByYear W28067673062021 @default.
• W2806767306 countsByYear W28067673062022 @default.
• W2806767306 crossrefType "journal-article" @default.
• W2806767306 hasAuthorship W2806767306A5025830431 @default.
• W2806767306 hasAuthorship W2806767306A5047255008 @default.
• W2806767306 hasAuthorship W2806767306A5057859275 @default.
• W2806767306 hasAuthorship W2806767306A5083043049 @default.
• W2806767306 hasBestOaLocation W28067673061 @default.
• W2806767306 hasConcept C126322002 @default.
• W2806767306 hasConcept C134018914 @default.
• W2806767306 hasConcept C142724271 @default.
• W2806767306 hasConcept C170493617 @default.
• W2806767306 hasConcept C176233148 @default.
• W2806767306 hasConcept C204787440 @default.
• W2806767306 hasConcept C2775864247 @default.
• W2806767306 hasConcept C2778514916 @default.
• W2806767306 hasConcept C2780764818 @default.
• W2806767306 hasConcept C2910564767 @default.
• W2806767306 hasConcept C31487548 @default.
• W2806767306 hasConcept C513476851 @default.
• W2806767306 hasConcept C71924100 @default.
• W2806767306 hasConcept C98274493 @default.
• W2806767306 hasConcept C99631742 @default.
• W2806767306 hasConceptScore W2806767306C126322002 @default.
• W2806767306 hasConceptScore W2806767306C134018914 @default.
• W2806767306 hasConceptScore W2806767306C142724271 @default.
• W2806767306 hasConceptScore W2806767306C170493617 @default.
• W2806767306 hasConceptScore W2806767306C176233148 @default.
• W2806767306 hasConceptScore W2806767306C204787440 @default.
• W2806767306 hasConceptScore W2806767306C2775864247 @default.
• W2806767306 hasConceptScore W2806767306C2778514916 @default.
• W2806767306 hasConceptScore W2806767306C2780764818 @default.
• W2806767306 hasConceptScore W2806767306C2910564767 @default.
• W2806767306 hasConceptScore W2806767306C31487548 @default.
• W2806767306 hasConceptScore W2806767306C513476851 @default.
• W2806767306 hasConceptScore W2806767306C71924100 @default.
• W2806767306 hasConceptScore W2806767306C98274493 @default.
• W2806767306 hasConceptScore W2806767306C99631742 @default.
• W2806767306 hasIssue "2" @default.
• W2806767306 hasLocation W28067673061 @default.
• W2806767306 hasLocation W28067673062 @default.

• next