FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2109307090> ?p ?o ?g. }

• W2109307090 endingPage "332" @default.
• W2109307090 startingPage "322" @default.
• W2109307090 abstract "4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1- (3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A), a new 2-aminothiazole derivative, shows nanomolar affinity for human cloned or native corticotrophin-releasing factor (CRF)(1) receptors (pK(i) values of 8.73 and 9.08, respectively), and a 1000-fold selectivity for CRF(1) versus CRF(2 alpha) receptor and CRF binding protein. SSR125543A antagonizes CRF-induced stimulation of cAMP synthesis in human retinoblastoma Y 79 cells (IC(50) = 3.0 +/- 0.4 nM) and adrenocorticotropin hormone (ACTH) secretion in mouse pituitary tumor AtT-20 cells. SSR125543A is devoid of agonist activity in these models. Its brain penetration was demonstrated in rats by using an ex vivo [(125)I-Tyr(0)] ovine CRF binding assay. SSR125543A displaced radioligand binding to the CRF(1) receptor in the brain with an ID(50) of 6.5 mg/kg p.o. (duration of action >24 h). SSR125543A also inhibited the increase in plasma ACTH levels elicited in rats by i.v. CRF (4 microg/kg) injection (ID(50) = 1, 5, or 5 mg/kg i.v., i.p., and p.o., respectively); this effect lasted for more than 6 h when the drug was given orally at a dose of 30 mg/kg. SSR125543A (10 mg/kg p.o.) reduced by 73% the increase in plasma ACTH levels elicited by a 15-min restraint stress in rats. Moreover, SSR125543A (20 mg/kg i.p.) also antagonized the increase of hippocampal acetylcholine release induced by i.c.v. injection of 1 microg of CRF in rats. Finally, SSR125543A reduced forepaw treading induced by i.c.v. injection of 1 microg of CRF in gerbils (ID(50) = approximately 10 mg/kg p.o.). Altogether, these data indicate that SSR125543A is a potent, selective, and orally active CRF(1) receptor antagonist." @default.
• W2109307090 created "2016-06-24" @default.
• W2109307090 creator A5001950169 @default.
• W2109307090 creator A5005748226 @default.
• W2109307090 creator A5008417197 @default.
• W2109307090 creator A5010860742 @default.
• W2109307090 creator A5018672429 @default.
• W2109307090 creator A5023364485 @default.
• W2109307090 creator A5031269524 @default.
• W2109307090 creator A5035552216 @default.
• W2109307090 creator A5036377365 @default.
• W2109307090 creator A5037480995 @default.
• W2109307090 creator A5037602051 @default.
• W2109307090 creator A5042093710 @default.
• W2109307090 creator A5046250589 @default.
• W2109307090 creator A5053122696 @default.
• W2109307090 creator A5056250454 @default.
• W2109307090 creator A5056345704 @default.
• W2109307090 creator A5056591563 @default.
• W2109307090 creator A5065591303 @default.
• W2109307090 creator A5067487520 @default.
• W2109307090 creator A5070809519 @default.
• W2109307090 creator A5073672761 @default.
• W2109307090 date "2002-04-01" @default.
• W2109307090 modified "2023-10-13" @default.
• W2109307090 title "4-(2-Chloro-4-methoxy-5-methylphenyl)-<i>N</i>-[(1<i>S</i>)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-<i>N</i>-(2-propynyl)-1,3-thiazol-2-amine Hydrochloride (SSR125543A): A Potent and Selective Corticotrophin-Releasing Factor₁Receptor Antagonist. I. Biochemical and Pharmacological Characterization" @default.
• W2109307090 cites W1951492130 @default.
• W2109307090 cites W1965874521 @default.
• W2109307090 cites W1967569415 @default.
• W2109307090 cites W1974253960 @default.
• W2109307090 cites W1977658029 @default.
• W2109307090 cites W1981304815 @default.
• W2109307090 cites W1981960003 @default.
• W2109307090 cites W1988230174 @default.
• W2109307090 cites W1989918919 @default.
• W2109307090 cites W1996096976 @default.
• W2109307090 cites W2005492092 @default.
• W2109307090 cites W2008776698 @default.
• W2109307090 cites W2023507956 @default.
• W2109307090 cites W2025906238 @default.
• W2109307090 cites W2034561886 @default.
• W2109307090 cites W2034584065 @default.
• W2109307090 cites W2043813981 @default.
• W2109307090 cites W2043915483 @default.
• W2109307090 cites W2052922750 @default.
• W2109307090 cites W2061599307 @default.
• W2109307090 cites W2066271355 @default.
• W2109307090 cites W2093260414 @default.
• W2109307090 cites W2095036452 @default.
• W2109307090 cites W2095646540 @default.
• W2109307090 cites W2098391261 @default.
• W2109307090 cites W2107337535 @default.
• W2109307090 cites W2120352095 @default.
• W2109307090 cites W2120835858 @default.
• W2109307090 cites W2124894806 @default.
• W2109307090 cites W2144044253 @default.
• W2109307090 cites W2156320778 @default.
• W2109307090 cites W2314976691 @default.
• W2109307090 cites W2322179823 @default.
• W2109307090 cites W27976590 @default.
• W2109307090 cites W2798061778 @default.
• W2109307090 cites W4376848280 @default.
• W2109307090 doi "https://doi.org/10.1124/jpet.301.1.322" @default.
• W2109307090 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11907190" @default.
• W2109307090 hasPublicationYear "2002" @default.
• W2109307090 type Work @default.
• W2109307090 sameAs 2109307090 @default.
• W2109307090 citedByCount "73" @default.
• W2109307090 countsByYear W21093070902012 @default.
• W2109307090 countsByYear W21093070902013 @default.
• W2109307090 countsByYear W21093070902014 @default.
• W2109307090 countsByYear W21093070902015 @default.
• W2109307090 countsByYear W21093070902016 @default.
• W2109307090 countsByYear W21093070902017 @default.
• W2109307090 countsByYear W21093070902021 @default.
• W2109307090 crossrefType "journal-article" @default.
• W2109307090 hasAuthorship W2109307090A5001950169 @default.
• W2109307090 hasAuthorship W2109307090A5005748226 @default.
• W2109307090 hasAuthorship W2109307090A5008417197 @default.
• W2109307090 hasAuthorship W2109307090A5010860742 @default.
• W2109307090 hasAuthorship W2109307090A5018672429 @default.
• W2109307090 hasAuthorship W2109307090A5023364485 @default.
• W2109307090 hasAuthorship W2109307090A5031269524 @default.
• W2109307090 hasAuthorship W2109307090A5035552216 @default.
• W2109307090 hasAuthorship W2109307090A5036377365 @default.
• W2109307090 hasAuthorship W2109307090A5037480995 @default.
• W2109307090 hasAuthorship W2109307090A5037602051 @default.
• W2109307090 hasAuthorship W2109307090A5042093710 @default.
• W2109307090 hasAuthorship W2109307090A5046250589 @default.
• W2109307090 hasAuthorship W2109307090A5053122696 @default.
• W2109307090 hasAuthorship W2109307090A5056250454 @default.
• W2109307090 hasAuthorship W2109307090A5056345704 @default.
• W2109307090 hasAuthorship W2109307090A5056591563 @default.
• W2109307090 hasAuthorship W2109307090A5065591303 @default.
• W2109307090 hasAuthorship W2109307090A5067487520 @default.
• W2109307090 hasAuthorship W2109307090A5070809519 @default.
• W2109307090 hasAuthorship W2109307090A5073672761 @default.
• W2109307090 hasConcept C126322002 @default.

• next