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Nepicastat hydrochloride (SYN117, RS-25560-197) is an inhibitor of dopamine beta-hydroxylase that catalyzes the conversion of dopamine to norepinephrine. Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity in vitro. In vivo, Nepicastat hydrochloride increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. Nepicastat is currently in Phase II clinical trials in patients with Posttraumatic Stress Disorder.
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| Animal Experiment | |
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| Animal models | spontaneously hypertensive rats (SHRs) |
| Formulation | water |
| Dosages | 3, 10, 30 or 100 mg/kg |
| Administration | p.o. |
| Molecular Weight | 331.81 |
| Formula | C14H15F2N3S.HCl |
| CAS Number | 170151-24-3 |
| Solubility (25°C) | DMSO 6 mg/mL Water 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Dopamine Receptor Products |
|---|
| Naxagolide
Naxagolide (Dopazinol) is a very potent and selective D2 agonist. |
| Alizapride hydrochloride
Alizapride hydrochloride is a dopamine receptor antagonist used for the theropy of nausea and vomiting. |
| Azaperone
Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic compound with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. |
| Benztropine mesylate
Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM. Benztropine mesylate is a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects. Benztropine mesylate is also an anti-histamine agent and a dopamine re-uptake inhibitor. |
| Bromocriptine Mesylate
Bromocriptine, an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes. |
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