| Identification | Back Directory | [Name]
1H-Indazole, 3-[5-[1-(3-methoxypropyl)-4-piperidinyl]-1,3,4-oxadiazol-2-yl]-1-(1-methylethyl)-, ethanedioate (1:1) | [CAS]
1428862-33-2 | [Synonyms]
Usmarapride
Usmarapride(SUVN-D4010)
1H-Indazole, 3-[5-[1-(3-methoxypropyl)-4-piperidinyl]-1,3,4-oxadiazol-2-yl]-1-(1-methylethyl)-, ethanedioate (1:1) | [Molecular Formula]
C23H31N5O6 | [MOL File]
1428862-33-2.mol | [Molecular Weight]
473.53 |
| Hazard Information | Back Directory | [Uses]
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease[1]. | [in vivo]
Usmarapride (SUVN-D4010) (1-3 mg/kg; p.o.; Male Wistar rats 10-12 weeks old) attenuates the long-term memory deficits in object recognition test (ORT)[1].
Usmarapride (1, 3, and 10 mg/kg; p.o.) significantly reverses the scopolamine-induced amnesia[1].
Usmarapride shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index[1].
Usmarapride (SUVN-D4010) shows good oral exposures, good bioavailability, and good brain exposures in rats[1].
Pharmacokinetic of Usmarapride in Rats[1]
(3.0 mg/kg for p.o. dosing; 1.0 mg/kg for i.v.)
| F% | Cmax (ng/mL) | AUC (ng·hr/mL) | t1/2 (h) | Vdss (L/kg) | CL (mLg/min/kg) | | 34 | 360 | 709 | 1.7 | 8.0 | 76 |
| [IC 50]
5-HT4 Receptor: 44 nM (EC50) | [References]
[1] Nirogi, Ramakrishna; Mohammed, Abdul Rasheed; Yarlgadda, Suresh; Ravella, Srinivasa Rao; Shinde, Anil Karbhari; Kambhampati, Ramasastri; Roayalley, Praveen Kumar; Jayarajan, Pradeep; Bhyrapuneni, Gopinadh; Patnala, Sriramachandra Murthy; et al. Preparatio |
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