| Stereochemistry | ABSOLUTE |
| Molecular Formula | C16H16N4O.ClH |
| Molecular Weight | 316.785 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C[C@@H](N)C1=CC=C(C=C1)C(=O)NC2=C3C=CNC3=NC=C2
InChI
InChIKey=IILQESWQPZIAGP-HNCPQSOCSA-N
InChI=1S/C16H16N4O.ClH/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15;/h2-10H,17H2,1H3,(H2,18,19,20,21);1H/t10-;/m1./s1
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| 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 |
| Molecular Formula | C16H16N4O |
| Molecular Weight | 280.3244 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Y-33075 is potent and selective ROCK (Rho-associated coiled-coil-forming protein kinase) inhibitor, developed by Yoshitomi Pharmaceutical Industries for encephalomyelitis treatment. In rabbits and in monkeys, Y-33075 lowers IOP in a dose-dependent fashion. An increase in regenerating axons of RGCs in 100 mM Y-33075-treated eyes is observed compared with saline-treated eyes. Y-33075 dose-dependently increases the number of RGCs with regenerating axons. Both Y-33075 induces a concentration-dependent relaxation in rabbit ciliary arteries precontracted with a high-potassium (high-K) solution. The amplitude of relaxation induced by Y-33075 is not affected by either 100 μM N (G)-nitro-L: -arginine methyl ester (L: -NAME) or 10 μM indomethacin. In Ca2 -free solution, Y-27632 and Y-39983 significantly inhibit the transient contraction of ciliary arteries induced by 10 μM histamine. However, neither Y-27632 nor Y-39983 affects the elevation of [Ca2 ](i) induced by high-K solution and histamine.
CNS Activity
Originator
Approval Year
Sourcing
PubMed
Sample Use Guides
Senju Pharmaceuticals completed a phase II trial that evaluated the dose-response relationship of ocular hypotensive efficacy and safety of Y 39983 at concentrations ranging from 0.003%, 0.01%, 0.03% or Y 39983 vehicle control given twice a day for 4 weeks in patients with primary open angle glaucoma or ocular hypertension (UMIN000018866)
Route of Administration:
Topical
