Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C14H16N2O4 |
| Molecular Weight | 276.2878 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(=O)N(O)[C@H]1[C@H](O)C(C)(C)OC2=CC=C(C=C12)C#N
InChI
InChIKey=IWTCFIIOUXJOOV-OLZOCXBDSA-N
InChI=1S/C14H16N2O4/c1-8(17)16(19)12-10-6-9(7-15)4-5-11(10)20-14(2,3)13(12)18/h4-6,12-13,18-19H,1-3H3/t12-,13+/m1/s1
Y-26763 is an active metabolite of Y-27152. Y-26763 is the novel K channel opener. It has been found to activate K channels in both cardiac myocytes and in smooth muscle cells from various tissues, suggesting that the compound has a non-specific effect on SUR1 and SUR2 channel subunits. Y-26763 well tolerated in healthy volunteers, and its pharmacologic effects were likely caused by vasodilation, which could make it an effective antihypertensive agent. At doses of 0.5 mg or higher, participants experienced headaches and palpitations, which were probably due to the vasodilatory effects and did not require treatment. Y-26763 partially protected against glycerol-induced acute renal failure. Also, it reduces infarct volume in focal cerebral ischemia in rats.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.1 ng/mL |
0.1 mg single, oral dose: 0.1 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
2.2 ng/mL |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
4.6 ng/mL |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.8 ng/mL |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
9.2 ng/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
6.1 ng/mL |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
59 ng × h/mL |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
105.6 ng × h/mL |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
156.9 ng × h/mL |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
186.1 ng × h/mL |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
144 ng × h/mL |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
16.8 h |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
14.2 h |
0.5 mg single, oral dose: 0.5 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
13 h |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
12.4 h |
1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
|
13.2 h |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
Y-26763 plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1 mg 1 times / day multiple, oral Highest studied dose Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: |
healthy |
Other AEs: headache... |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| headache | 1 mg 1 times / day multiple, oral Highest studied dose Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: |
healthy |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Long-term effects of benidipine on cerebral vasoreactivity in hypertensive rats. | 2002-03-08 |
|
| Role of potassium channels in halothane-epinephrine arrhythmias. | 1998-06 |
|
| Age-related changes in response of brain stem vessels to opening of ATP-sensitive potassium channels. | 1997-01 |
|
| Y-26763 protects the working rat myocardium from ischemia/reperfusion injury through opening of KATP channels. | 1996-12-19 |
|
| Altered cerebrovascular response to a potassium channel opener in hypertensive rats. | 1996-07 |
|
| Effects of Y-26763, a novel K-channel opener, on electrical responses of smooth muscles in the guinea pig bladder. | 1996-04 |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Y-27152 itself is pharmacologically inert and is converted to its active form, Y-26763, after oral administration.
In the first phase, single doses of 0.1, 0.25, 0.5, 0.75, and 1.0 mg of Y-27152 were given after overnight fasts in a dose-escalating manner. The 0.75-mg dose was given both after an overnight fast or after food to examine the effects of food intake. In the second phase, multiple doses of Y-27152 were taken after meals once daily for 7 consecutive days. In part A of this phase, either placebo or 0.5 mg of Y-27152 was taken for 7 days, and in part B of this phase 0.5-, 0.75-, and 1.0-mg doses were taken in a dose-escalating manner for 1,3, and 3 days, respectively.
Route of Administration:
Oral
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Q9F3XV8A6X
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DTXSID80155562
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127408-31-5
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121878
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ACTIVE MOIETY
PARENT (METABOLITE ACTIVE)
