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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
Structure of P-1075

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)

HIDE SMILES / InChI

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

Targets

Primary TargetPharmacologyConditionPotency
21.88 nM [EC50]
230.0 nM [EC50]
21.88 nM [EC50]
PubMed

PubMed

TitleDatePubMed
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 Mon Mar 31 18:07:48 GMT 2025
Edited
by admin
on Mon Mar 31 18:07:48 GMT 2025
Record UNII
RA77IZ6B2F
Record Status Validated (UNII)
Record Version
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Name Type Language
P 1075
Preferred Name English
P-1075
Code English
P1075
Code English
N-CYANO-N'-(1,1-DIMETHYL-PROPYL)-N''-3-PYRIDINYL GUANIDINE
Systematic Name English
U-83757
Code English
PNU-83757
Code English
GUANIDINE, N-CYANO-N'-(1,1-DIMETHYLPROPYL)-N''-3-PYRIDINYL-
Systematic Name English
Code System Code Type Description
PUBCHEM
43345
Created by admin on Mon Mar 31 18:07:48 GMT 2025 , Edited by admin on Mon Mar 31 18:07:48 GMT 2025
PRIMARY
FDA UNII
RA77IZ6B2F
Created by admin on Mon Mar 31 18:07:48 GMT 2025 , Edited by admin on Mon Mar 31 18:07:48 GMT 2025
PRIMARY
CAS
60559-98-0
Created by admin on Mon Mar 31 18:07:48 GMT 2025 , Edited by admin on Mon Mar 31 18:07:48 GMT 2025
PRIMARY
EPA CompTox
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
PRIMARY
Related Record Type Details
TARGET -> ACTIVATOR
Potassium channel opener
Related Record Type Details
ACTIVE MOIETY