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Ispronicline

Names

[ CAS No. ]:
252870-53-4

[ Name ]:
Ispronicline

[Synonym ]:
UNII-3E05NBH9V5
(2S)-(4E)-N-methyl-5-[5-isopropoxypyridin-3-yl]-4-penten-2-amine
(2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridinyl)-4-penten-2-amine
(2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine
(2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine
Ispronicline
AZD-3480
RJR-1734
Ispronicline (INN/USAN)

Biological Activity

[Description]:

Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR
Signaling Pathways >> Neuronal Signaling >> nAChR
Research Areas >> Neurological Disease

[In Vivo]

Ispronicline (10-20 mg/kg; s.c.) induces c-Fos expression in selective regions of the rat forebrain[1]. Ispronicline pharmacokinetics (half-life of 2 h in rats) contrasts with the long-lasting improvement of working memory (18 h to 2 d)[2]. Animal Model: Male Wistar rats weighting 180-200 g[1] Dosage: 10 and 30 mg/kg Administration: s.c. Result: Induced c-Fos in medial paraventricular nucleus of hypothalamus. Treatment with 30 mg/kg ispronicline, but not 10 mg/kg, increased the number of c-Fos immunoreactive cells significantly as compared to controls within the medial parvocellular part of paraventricular nucleus (PVN).

[References]

[1]. Julie Jacobsen, et al. The α4β2 nicotine acetylcholine receptor agonist ispronicline induces c-Fos expression in selective regions of the rat forebrain. Neurosci Lett. 2012 Apr 25;515(1):7-11.

Chemical & Physical Properties

[ Molecular Formula ]:
C14H22N2O

[ Molecular Weight ]:
234.34

[ Exact Mass ]:
234.17300

[ PSA ]:
34.15000

[ LogP ]:
3.27090

[ Storage condition ]:
-20°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds