Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C27H32FN5O4 |
| Molecular Weight | 509.5725 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(OC)C(C2=CC=C(F)C=C2)=C3C(N)=CC(=NC3=C1)N4CCCN(CC4)C(=O)N5CCOCC5
InChI
InChIKey=IHSGHTLNHSMKII-UHFFFAOYSA-N
InChI=1S/C27H32FN5O4/c1-35-22-17-21-25(24(26(22)36-2)18-4-6-19(28)7-5-18)20(29)16-23(30-21)31-8-3-9-32(11-10-31)27(34)33-12-14-37-15-13-33/h4-7,16-17H,3,8-15H2,1-2H3,(H2,29,30)
| Molecular Formula | C27H32FN5O4 |
| Molecular Weight | 509.5725 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Nonlinear oral pharmacokinetics of the alpha-antagonist 4-amino-5-(4-fluorophenyl)-6,7-dimethoxy-2-[4-(morpholinocarbonyl)-perhydro-1,4-diazepin-1-yl]quinoline in humans: use of preclinical data to rationalize clinical observations. | 2004 Feb |
|
| Impact of physicochemical and structural properties on the pharmacokinetics of a series of alpha1L-adrenoceptor antagonists. | 2007 Aug |
|
| In vivo performance of an oral MR matrix tablet formulation in the beagle dog in the fed and fasted state: assessment of mechanical weakness. | 2008 May |
|
| Scintigraphic study to investigate the effect of food on a HPMC modified release formulation of UK-294,315. | 2009 Apr |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 18:28:26 GMT 2023
by
admin
on
Sat Dec 16 18:28:26 GMT 2023
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| Record UNII |
TT7PL9XFE2
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| Record Status |
Validated (UNII)
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| Record Version |
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192868-49-8
Created by
admin on Sat Dec 16 18:28:26 GMT 2023 , Edited by admin on Sat Dec 16 18:28:26 GMT 2023
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TT7PL9XFE2
Created by
admin on Sat Dec 16 18:28:26 GMT 2023 , Edited by admin on Sat Dec 16 18:28:26 GMT 2023
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10279136
Created by
admin on Sat Dec 16 18:28:26 GMT 2023 , Edited by admin on Sat Dec 16 18:28:26 GMT 2023
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Chemical synthesis of UK-294315.
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ACTIVE MOIETY |
(UK-294,315) is an antagonist of the human alpha1-adrenoceptor and exhibits nonlinear oral pharmacokinetics in humans. Oral absorption in humans is extensive, with only 14% of an orally administered (20 mg) radiolabeled dose excreted unchanged in the feces. In rats and dogs, UK-294,315 is partially eliminated as unchanged drug in feces (29 and 14% of an intravenous dose, respectively). Oral bioavailability is low in rats (11%) and high in dogs (71%), in keeping with systemic clearance. Fecal elimination of unchanged drug was 60% after oral administration to rats, indicating incomplete absorption in this species, whereas absorption in dogs is complete. UK-294,315 is a P-glycoprotein (P-gp) substrate (Km, 15 microM) exhibiting polarized flux in Caco-2 cell monolayers, saturable across a concentration range of 5 to 200 microM.
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