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| | Nepicastat hydrochloride Basic information |
| Product Name: | Nepicastat hydrochloride | | Synonyms: | NEPICASTAT HYDROCHLORIDE;Nepicastat HCl (SYN-117),Nepicastat hydrochloride,;Nepicastat (SYN-117) HCl;Nepicastat HCl (SYN-117);4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione;(S)-5-(AMinoMethyl)-1-(5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)-1H-iMidazole-2(3H)-thione hydrochloride;Nepicastat (SYN117)HCI;RS 25560-197 Nepicastat hydrochloride | | CAS: | 170151-24-3 | | MF: | C14H16ClF2N3S | | MW: | 331.81 | | EINECS: | | | Product Categories: | Inhibitors;Inhibitor | | Mol File: | 170151-24-3.mol |  |
| | Nepicastat hydrochloride Chemical Properties |
| storage temp. | Inert atmosphere,Store in freezer, under -20°C | | solubility | DMSO: soluble10mg/mL, clear | | form | powder | | color | white to beige | | InChIKey | DIPDUAJWNBEVOY-PPHPATTJSA-N |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26 | | WGK Germany | 3 |
| | Nepicastat hydrochloride Usage And Synthesis |
| Description | Nepicastat is an inhibitor of dopamine β-hydroxylase (DBH; IC50 = 9 nM for the purified human enzyme). It is selective for DBH over a panel of 12 enzymes and 13 neurotransmitter receptors (IC50s or Kis = >10 μM). Nepicastat dose-dependently reduces norepinephrine content and increases dopamine content in the mesenteric artery, left ventricle, and cerebral cortex in spontaneously hypertensive rats, as well as in the renal artery, left ventricle, and cerebral cortex in beagle dogs. It attenuates increases in diastolic blood pressure and heart rate induced by preganglionic sympathetic nerve stimulation in pithed spontaneously hypertensive rats when administered orally at doses of 10 and 30 mg/kg. Nepicatstat (50 mg/kg) reduces the progressive ratio response for cocaine, but not food or sucrose pellets, in rats. It also reduces reinstatement of cocaine-seeking behavior induced by cues, yohimbine , or foot-shock in rats. | | Uses | Nepicastat Hydrochloride is a potent and selective dopamine β-hydrolase inhibitor. Used in cardiovascular treatment where deficiencies in ventricles results in heart failure. | | storage | Store at -20°C | | references | [1]. stanley wc, li b, bonhaus dw, et al. catecholamine modulatory effects of nepicastat (rs-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. br j pharmacol, 1997, 121(8): 1803-1809.
[2]. stanley wc, lee k, johnson lg, et al. cardiovascular effects of nepicastat (rs-25560-197), a novel dopamine beta-hydroxylase inhibitor. j cardiovasc pharmacol, 1998, 31(6): 963-970.
[3]. devoto p, flore g, saba p, et al. the dopamine beta-hydroxylase inhibitor nepicastat increases dopamine release and potentiates psychostimulant-induced dopamine release in the prefrontal cortex. addict biol, 2014, 19(4): 612-622. |
| | Nepicastat hydrochloride Preparation Products And Raw materials |
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