Donitriptan hydrochloride is a potent, selective, high-efficacy agonist at 5-HT1B/1D receptors both in vivo and in vitro in neuronal and vascular models relevant to migraine. Donitriptan hydrochloride has subnanomolar affinity for cloned human and nonhuman 5-HT1B and 5-HT1D receptors with Ki values ranging from 0.1-4.3 nM. It potently inhibits forskolin-induced cAMP accumulation mediated by recombinant human and nonhuman, stably transfected 5-HT1B and 5-HT1D receptors with mean EC50 values ranging from 0.2-1.9 nM . In mammals, 5-hydroxytryptamine (5-HT) is important in regulating emotions and related behaviors as a neurotransmitter . In C6 glioma cells transfected with human 5-HT1B or 5-HT1D receptors, donitriptan hydrochloride enhanced specific GTPγ35S binding at both 5-HT1B and 5-HT1D receptors to a greater extent, compared with rizatriptan, naratriptan, sumatriptan, dihydroergotamine and zolmitriptan, but to a level equivalent to which evoked by 5-HT. In guinea pig-isolated trigeminal ganglion neurons, treatment with donitriptan hydrochloride resulted in increase in Ca2+-dependent K+ current (pD2 = 7.3) . Oral administration with donitriptan hydrochloride in guinea pigs resulted in hypothermic responses with an ED50 of 1.6 mg/kg. Compared with zolmitriptan, naratriptan and rizatriptan with an ED50 of 8.3, 9.9 and 12.3 mg/kg, respectively, donitriptan hydrochloride showed superior potency. There is likelihood that donitriptan hydrochloride gains access to the brain .Donitriptan hydrochloride is orally active and well tolerated by animals, displays unique craniovascular selectivity and a long duration of action, and gains access to the brain.

Product information

CAS Number: 170911-68-9

Molecular Weight: 439.94

Formula: C23H26ClN5O2

Chemical Name: 4-[4-(2-{[3-(2-aminoethyl)-1H-indol-5-yl]oxy}acetyl)piperazin-1-yl]benzonitrile hydrochloride

Smiles: Cl.NCCC1=CNC2=CC=C(C=C21)OCC(=O)N1CCN(CC1)C1C=CC(=CC=1)C#N

InChiKey: ZXENQGQAPOYDOJ-UHFFFAOYSA-N

InChi: InChI=1S/C23H25N5O2.ClH/c24-8-7-18-15-26-22-6-5-20(13-21(18)22)30-16-23(29)28-11-9-27(10-12-28)19-3-1-17(14-25)2-4-19;/h1-6,13,15,26H,7-12,16,24H2;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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