H-89
Names | |
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IUPAC name
N-[2-[[3-(4-Bromophenyl)-2-propenyl]amino]ethyl]-5-isoquinolinesulfonamide | |
Identifiers | |
127243-85-0 | |
3D model (Jmol) | Interactive image |
ChEBI | CHEBI:47495 |
ChEMBL | ChEMBL104264 |
ChemSpider | 395827 |
ECHA InfoCard | 100.201.023 |
5983 | |
PubChem | 449241 |
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Properties | |
C20H20BrN3O2S | |
Molar mass | 446.36 g·mol−1 |
Soluble to 25 mM in Water | |
Solubility | up to 100 mM DMSO |
Hazards | |
Main hazards | Exposure may cause irritation to eyes, mucous membranes, upper
respiratory tract and skin. |
S-phrases | S22 - Do not breathe dust S24/25 - Avoid contact with skin and eyes S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
verify (what is ?) | |
Infobox references | |
H-89 is a Protein kinase A inhibitor that also inhibits several other kinases (IC50 values are 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b).[1][2] H-89 blocks PKA actions through competitive inhibition of the adenosine triphosphate (ATP) site on the PKA catalytic subunit.[3]
H-89 and seizure
Recent study showed that using H-89 in the pentylenetetrazol-induced seizure in the wild type mice increase seizure threshold and latency.[4]
H-89 and morphine withdrawal syndrome
The effect of H-89 (0.5, 1, 5 mg/kg) has been studied in morphine withdrawal syndrome in wild-type mice. The results indicated that H-89 significantly reduced the morphine withdrawal syndrome. In addition, results show that combination of H-89 with bucladesine as a cAMP analog has a additive attenuating effect on morphine withdrawal syndrome [5]
References
- ↑ Marunaka, Yoshinori; Niisato, Naomi (2003). "H89, an inhibitor of protein kinase A (PKA), stimulates Na+ transport by translocating an epithelial Na+ channel (ENaC) in fetal rat alveolar type II epithelium". Biochemical Pharmacology. 66 (6): 1083–9. doi:10.1016/S0006-2952(03)00456-8. PMID 12963496.
- ↑ Lochner, A.; Moolman, J. A. (2006). "The Many Faces of H89: A Review". Cardiovascular Drug Reviews. 24 (3–4): 261–74. doi:10.1111/j.1527-3466.2006.00261.x. PMID 17214602.
- ↑ Murray, A. J. (2008). "Pharmacological PKA Inhibition: All May Not Be What It Seems". Science Signaling. 1 (22): re4. doi:10.1126/scisignal.122re4. PMID 18523239.
- ↑ Hosseini-Zare, Mahshid Sadat; Salehi, Forouz; Seyedi, Seyedeh Yalda; Azami, Kian; Ghadiri, Tahereh; Mobasseri, Mohammad; Gholizadeh, Shervin; Beyer, Cordian; Sharifzadeh, Mohammad (2011). "Effects of pentoxifylline and H-89 on epileptogenic activity of bucladesine in pentylenetetrazol-treated mice". European Journal of Pharmacology. 670 (2–3): 464–70. doi:10.1016/j.ejphar.2011.09.026. PMID 21946102.
- ↑ Seyedi, Seyedeh Y.; Salehi, Forouz; Payandemehr, Borna; Hossein, Sara; Hosseini-Zare, Mahshid S.; Nassireslami, Ehsan; Yazdi, Behnoosh B.; Sharifzadeh, Mohammad (2014). "Dual effect of cAMP agonist on ameliorative function of PKA inhibitor in morphine-dependent mice". Fundamental & Clinical Pharmacology. 28 (4): 445–54. doi:10.1111/fcp.12045. PMID 24033391.