Usmarapride free base

Names

[ Name ]:
Usmarapride free base

[Synonym ]:
1H-Indazole, 3-[5-[1-(3-methoxypropyl)-4-piperidinyl]-1,3,4-oxadiazol-2-yl]-1-(1-methylethyl)-
1-Isopropyl-3-{5-[1-(3-methoxypropyl)-4-piperidinyl]-1,3,4-oxadiazol-2-yl}-1H-indazole
GNQ25KYD72

Biological Activity

[Description]:

Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT4 Receptor:44 nM (EC50)

[In Vivo]

Usmarapride (SUVN-D4010) (1-3 mg/kg; p.o.; Male Wistar rats 10-12 weeks old) free base attenuates the long-term memory deficits in object recognition test (ORT)[1]. Usmarapride (1, 3, and 10 mg/kg; p.o.) free base significantly reverses the scopolamine-induced amnesia[1]. Usmarapride free base shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index[1]. Usmarapride (SUVN-D4010) free base shows good oral exposures, good bioavailability, and good brain exposures in rats[1].

[References]

[1]. Nirogi R, et al. Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT4 Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer's Disease. J Med Chem. 2021;64(15):10641-10665.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
541.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₂₉N₅O₂

[ Molecular Weight ]:
383.487

[ Flash Point ]:
281.5±32.9 °C

[ Exact Mass ]:
383.232117

[ LogP ]:
1.78

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.636

Related Compounds

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