PiMobendan (hydrochloride) manufacturers
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| | PiMobendan (hydrochloride) Basic information |
| Product Name: | PiMobendan (hydrochloride) | | Synonyms: | PiMobendan (hydrochloride);4,5-Dihydro-6-[2-(4-methoxyphenyl)-1H-benzimidazol-5-yl]-5-methyl-3(2H)-pyridazinone monohydrochloride;6-[2-(4-Methoxyphenyl)-1H-1,3-benzodiazol-6-yl]-5-methyl-2,3,4,5-tetrahydropyridazin-3-one hydrochloride | | CAS: | 77469-98-8 | | MF: | C19H19ClN4O2 | | MW: | 370.83276 | | EINECS: | | | Product Categories: | | | Mol File: | 77469-98-8.mol |  |
| | PiMobendan (hydrochloride) Chemical Properties |
| Melting point | 311°(dec) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder |
| Toxicity | LD50 orally in mice: ~600 mg/kg (Austel, 1982) |
| | PiMobendan (hydrochloride) Usage And Synthesis |
| Uses | Pimobendan hydrochloride (UD-CG115 hydrochloride) is a selective inhibitor of PDE3 with IC50 of 0.32 μM. | | Biological Activity | Pimobendan hydrochloride (UD-CG115 hydrochloride) is a selective inhibitor of PDE3 with IC50 of 320 nM. | | in vitro | Pimobendan hydrochloride (UD-CG115 hydrochloride) exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC 50 of 0.32 uM compared to the inhibition of PDE I and PDE II ( IC 50 >30 μM). In human atrial cells, 100 μM Pimobendan (UD-CG115) significantly increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC 50 ) of 1.13 μM. In rabbit atrial cells, Pimobendan (UD-CG115) increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells. | | in vivo | Pimobendan (UD-CG115) shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan (UD-CG115) significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). It (UD-CG115) (1 mg/kg) also significantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with the control group, which shows no effect on myocardial necrosis, heart weight and body weight. Pimobendan (UD-CG115) suppresses expression of the intracardiac iNOS gene , causing reduction of intracardiac NO production. | | References | [1] Kajimoto K, et al. Contribution of phosphodiesterase isozymes to the regulation of the L-type calcium current in human cardiac myocytes. Br J Pharmacol. 1997 Aug;121(8):1549-56. DOI:10.1038/sj.bjp.0701297
[2] Iwasaki A, et al. Pimobendan inhibits the production of proinflammatory cytokines and gene expression of inducible nitric oxide synthase in a murine model of viral myocarditis. J Am Coll Cardiol. 1999 Apr;33(5):1400-7. DOI:10.1016/s0735-1097(98)00692-5 |
| | PiMobendan (hydrochloride) Preparation Products And Raw materials |
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