LEVCROMAKALIM

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C16H18N2O3
Molecular Weight	286.3257
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC1(C)OC2=C(C=C(C=C2)C#N)[C@H]([C@@H]1O)N3CCCC3=O

InChI

InChIKey=TVZCRIROJQEVOT-CABCVRRESA-N

InChI=1S/C16H18N2O3/c1-16(2)15(20)14(18-7-3-4-13(18)19)11-8-10(9-17)5-6-12(11)21-16/h5-6,8,14-15,20H,3-4,7H2,1-2H3/t14-,15+/m1/s1

HIDE SMILES / InChI

Molecular Formula	C16H18N2O3
Molecular Weight	286.3257
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description

Cromakalim is an ATP-sensitive potassium (KATP) channel opener, which was studied for the treatment of gastric ulcer, hypertension and preventing a cardiomyopathy. But the development of this drug was discontinued due to heart lesions found in monkey chronic toxicity studies.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Sulfonylurea receptor 2 9	Opener 34		7.12 null [pKi]
ATP-sensitive potassium (KATP) channel 4	Opener 34

Conditions

Condition	Modality	Highest Phase	Product
Hypertension 567	Primary	Preclinical	Unknown
Asthma 241	Primary	Preclinical	Unknown
Gastric ulcer 67	Primary	Withdrawn	Unknown
Cardiomyopathy 21	Preventing	Withdrawn	Unknown
Hypertension 567	Primary	Withdrawn	Unknown

PubMed

Show entries

Title	Date	PubMed
The relaxant action of BRL 34915 in rat uterus.	1987 Aug	2444298
Preclinical pharmacology of Ro 31-6930, a new potassium channel opener.	1990 Feb	1689412
Effects of potassium channel modulation during global ischaemia in isolated rat heart with and without cardioplegia.	1992 Nov	1291083
K+ channel openers delay intestinal transit and have antidiarrheal activity.	1995 Dec 12	8749038
Glibenclamide-sensitive hypotension produced by helodermin assessed in the rat.	1998 Dec	9881641