Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H17N5 |
| Molecular Weight | 231.2969 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC(C)(C)NC(NC1=CC=CN=C1)=NC#N
InChI
InChIKey=HKZNADVVGXKQDL-UHFFFAOYSA-N
InChI=1S/C12H17N5/c1-4-12(2,3)17-11(15-9-13)16-10-6-5-7-14-8-10/h5-8H,4H2,1-3H3,(H2,15,16,17)
| Molecular Formula | C12H17N5 |
| Molecular Weight | 231.2969 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2095198 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17154517 |
21.88 nM [EC50] | ||
Target ID: CHEMBL1971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19101153 |
230.0 nM [EC50] | ||
Target ID: CHEMBL2095152 |
21.88 nM [EC50] |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Substitution of the Walker A lysine by arginine in the nucleotide-binding domains of sulphonylurea receptor SUR2B: effects on ligand binding and channel activity. | 2010-06 |
|
| Syntaxin-1A inhibition of P-1075, cromakalim, and diazoxide actions on mouse cardiac ATP-sensitive potassium channel. | 2008-12-01 |
|
| Potassium fluxes, energy metabolism, and oxygenation in intact diabetic rat hearts under normal and stress conditions. | 2008-10 |
|
| Three C-terminal residues from the sulphonylurea receptor contribute to the functional coupling between the K(ATP) channel subunits SUR2A and Kir6.2. | 2008-07-01 |
|
| K(ATP) channel expression and pharmacological in vivo and in vitro studies of the K(ATP) channel blocker PNU-37883A in rat middle meningeal arteries. | 2008-05 |
|
| GSK3beta inhibition and K(ATP) channel opening mediate acute opioid-induced cardioprotection at reperfusion. | 2007-07 |
|
| Pharmacological characterization of urinary bladder smooth muscle contractility following partial bladder outlet obstruction in pigs. | 2006-02-17 |
|
| P-1075 exerts diverse modulatory effects on mitochondrial ATP-sensitive K+ channels in rabbit ventricular myocytes. | 2006-02 |
|
| Characterization of K(ATP)-channels in rat basilar and middle cerebral arteries: studies of vasomotor responses and mRNA expression. | 2005-10-31 |
|
| Reduced effectiveness of HMR 1098 in blocking cardiac sarcolemmal K(ATP) channels during metabolic stress. | 2005-10 |
|
| Lipids modulate ligand binding to sulphonylurea receptors. | 2005-08 |
|
| Effect of thimerosal on arrhythmia induced by coronary ligation: the involvement of ATP-dependent potassium channels. | 2005-07 |
|
| Alteration of binding sites for [3H]P1075 and [3H]glibenclamide in renovascular hypertensive rat aorta. | 2005-01 |
|
| Identification and pharmacological characterization of sarcolemmal ATP-sensitive potassium channels in the murine atrial HL-1 cell line. | 2005-01 |
|
| In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892. | 2004-09 |
|
| Interaction of a novel dihydropyridine K+ channel opener, A-312110, with recombinant sulphonylurea receptors and KATP channels: comparison with the cyanoguanidine P1075. | 2004-04 |
|
| Sarcolemmal and mitochondrial effects of a KATP opener, P-1075, in "polarized" and "depolarized" Langendorff-perfused rat hearts. | 2003-12-03 |
|
| P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts. | 2003-09 |
|
| Selective ATP-sensitive potassium channel openers: fact or fiction. | 2003-09 |
|
| Cardioselective sulfonylthiourea HMR 1098 blocks mitochondrial uncoupling induced by a KATP channel opener, P-1075, in beating rat hearts. | 2003-07-14 |
|
| [125I]A-312110, a novel high-affinity 1,4-dihydropyridine ATP-sensitive K+ channel opener: characterization and pharmacology of binding. | 2003-07 |
|
| Binding and effect of K ATP channel openers in the absence of Mg2+. | 2003-05 |
|
| PNU-83757: a new agent for the treatment of erectile dysfunction. | 2002-12 |
|
| Development of a sensitive bioanalytical method for determination of PNU-83757 in rat, monkey and human plasma: from LC-UV to LC-MS/MS. | 2002-10-15 |
|
| Fluorescence-based functional assay for sarcolemmal ATP-sensitive potassium channel activation in cultured neonatal rat ventricular myocytes. | 2002-08-08 |
|
| Structure-Activity studies for a novel series of tricyclic dihydropyrimidines as K(ATP) channel openers (KCOs). | 2002-06-03 |
|
| The efficacy, safety and tolerability of intracavernous PNU-83757 for the treatment of erectile dysfunction. | 2002-06 |
|
| Effects of K(ATP) channel openers, P-1075, pinacidil, and diazoxide, on energetics and contractile function in isolated rat hearts. | 2002-04 |
|
| KCO912: a potent and selective opener of ATP-dependent potassium (K(ATP)) channels which suppresses airways hyperreactivity at doses devoid of cardiovascular effects. | 2002-03 |
|
| Interaction of K(ATP) channel modulators with sulfonylurea receptor SUR2B: implication for tetramer formation and allosteric coupling of subunits. | 2002-02 |
|
| Characterization of a mutant sulfonylurea receptor SUR2B with high affinity for sulfonylureas and openers: differences in the coupling to Kir6.x subtypes. | 2001-07 |
|
| Functional implication of spare ATP-sensitive K(+) channels in bladder smooth muscle cells. | 2001-03 |
|
| Pharmacological comparison of native mitochondrial K(ATP) channels with molecularly defined surface K(ATP) channels. | 2001-02 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:07:48 GMT 2025
by
admin
on
Mon Mar 31 18:07:48 GMT 2025
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| Record UNII |
RA77IZ6B2F
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| Record Status |
Validated (UNII)
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| Record Version |
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43345
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RA77IZ6B2F
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60559-98-0
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DTXSID60209335
Created by
admin on Mon Mar 31 18:07:48 GMT 2025 , Edited by admin on Mon Mar 31 18:07:48 GMT 2025
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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TARGET -> ACTIVATOR |
Potassium channel opener
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
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