UK-357903

Details

Stereochemistry	ACHIRAL
Molecular Formula	C27H34N8O5S
Molecular Weight	582.674
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCN1CCN(CC1)S(=O)(=O)C2=CN=C(OCCOC)C(=C2)C3=NC4=C(CC)N(CC5=CC=CC=N5)N=C4C(=O)N3

InChI

InChIKey=QDPNAMRLQRQPMR-UHFFFAOYSA-N

InChI=1S/C27H34N8O5S/c1-4-22-23-24(32-35(22)18-19-8-6-7-9-28-19)26(36)31-25(30-23)21-16-20(17-29-27(21)40-15-14-39-3)41(37,38)34-12-10-33(5-2)11-13-34/h6-9,16-17H,4-5,10-15,18H2,1-3H3,(H,30,31,36)

HIDE SMILES / InChI

Molecular Formula	C27H34N8O5S
Molecular Weight	582.674
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Substance Class	Chemical
Record UNII	D36Q3E2UUJ
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

UK-357903

Code

English

PIPERAZINE, 1-ETHYL-4-((5-(3-ETHYL-4,7-DIHYDRO-7-OXO-2-(2-PYRIDINYLMETHYL)-2H-PYRAZOLO(4,3-D)PYRIMIDIN-5-YL)-6-(2-METHOXYETHOXY)-3-PYRIDINYL)SULFONYL)-

Systematic Name

English

7H-PYRAZOLO(4,3-D)PYRIMIDIN-7-ONE, 3-ETHYL-5-(5-((4-ETHYL-1-PIPERAZINYL)SULFONYL)-2-(2-METHOXYETHOXY)-3-PYRIDINYL)-2,6-DIHYDRO-2-(2-PYRIDINYLMETHYL)-

Systematic Name

English

3-ETHYL-5-(5-(4-ETHYLPIPERAZIN-1-YL)SULFONYL-2-(2-METHOXYETHOXY)-3-PYRIDYL)-2-(2-PYRIDYLMETHYL)-6H-PYRAZOLO(4,3-D)PYRIMIDIN-7-ONE

Systematic Name

English

UK357903

Code

English

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Code System

Code

Type

Description

PUBCHEM

135456180

PRIMARY

CAS

247580-98-9

PRIMARY

FDA UNII

D36Q3E2UUJ

PRIMARY

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Related Record

Type

Details


					D36Q3E2UUJ

UK-357903

ACTIVE MOIETY

Comments:

Structure of UK-357,903 and IC50 values for inhibition of phosphodiesterase (PDE) enzymes. Enzyme: PDE5, PDE6a, PDE1-3 and 7-11; Geometric mean IC50 (nM) (nX3) 95% CI; PDE5 1.3 (1.11.6); PDE6a 714 (575887); PDE1-3 and 7-11 410,000


					D36Q3E2UUJ

UK-357903

ACTIVE MOIETY

Comments:

Mechanism of Action: Type 5 cyclic nucleotide phosphodiesterase inhibitor; Highest Development Phase: Discontinued for Erectile dysfunction; Most Recent Event: 05 Sep 2006 Discontinued - Phase-II for Erectile dysfunction in Europe (unspecified route)


					D36Q3E2UUJ

UK-357903

ACTIVE MOIETY

Comments:

Nitric oxide is the main inhibitory neurotransmitter in the internal anal sphincter. UK 357,903 (an inhibitor of type-5 phosphodiesterase (PDE)) prevents hydrolysis of cyclic guanosine monophosphate, enhancing the effect of nitric oxide.


					D36Q3E2UUJ

UK-357903

ACTIVE MOIETY

Comments:

The regional hemodynamic responses to continuous 4-day infusion of UK-357,903 (266 microg kg(-1) h(-1)) alone and in combination with a low dose of enalapril (10 microg kg(-1) h(-1)) were measured in conscious spontaneously hypertensive rats to test the hypothesis that the renin-angiotensin system may influence the cardiovascular consequences of inhibition of phosphodiesterase 5 (PDE5) by UK-357,903 or vice versa. UK-357,903 alone caused a fall in mean blood pressure (-12.1 mm Hg) associated with vasodilatation in the mesenteric and hindquarters vascular beds.

Showing 1 to 4 of 4 entries

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