2414674-71-6

2414674-71-6 structure

Name: SUVN-911(compound 9h)
Chemical Name: SUVN-911
CAS Number: 2414674-71-6
Molecular Formula: C₁₁H₁₄Cl₂N₂O
Molecular Weight: 261.15
Catalog: Signaling Pathways Membrane Transporter/Ion Channel nAChR
Create Date: 2020-06-01 14:19:09
Modify Date: 2024-01-14 20:45:14
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity[1].

Name	SUVN-911

Description	SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR Signaling Pathways >> Neuronal Signaling >> nAChR Research Areas >> Neurological Disease
Target	Ki: 1.5 nM (α4β2 receptor)[1]
In Vitro	SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR[1]. SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins[1].
In Vivo	SUVN-911 is devoid of cardiovascular and gastrointestinal side effects[1]. SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects[1]. SUVN-911 shows metabolic stability in rats[1]. SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats[1]. Animal Model: Male Wistar rats (180-230 g)[1] Dosage: 1 mg/kg, 3 mg/kg, 10.0 mg/kg Administration: Oral administration, daily, for 3 days Result: Showed antidepressant like activity with no signs of tachyphylaxis. Animal Model: Male Wistar rats (225 ± 25 gm)[1] Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=3507 ng*h/mL, T1/2=3.34 hours.
References	[1]. Ramakrishna Nirogi, et al. Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression. J Med Chem. 2020 Mar 26;63(6):2833-2853.

Molecular Formula	C₁₁H₁₄Cl₂N₂O
Molecular Weight	261.15

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