SIB-1553A

Names

[ CAS No. ]:
191611-89-9

[ Name ]:
SIB-1553A

[Synonym ]:
Phenol, 4-[[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]-, hydrochloride (1:1)
4-{[2-(1-Methyl-2-pyrrolidinyl)ethyl]sulfanyl}phenol hydrochloride (1:1)

Biological Activity

[Description]:

SIB-1553A hydrochloride is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A hydrochloride is also a selective neuronal nAChR ligand. SIB-1553A hydrochloride is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[In Vitro]

SIB-1553A hydrochloride displaces the binding of [H]nicotine (NIC) to the rat brain nAChRs with an IC50 value of 110 nM[1]. In calcium flux assays, SIB-1553A hydrochloride (0.1-5 μM), shows a greater selectivity for beta4-subunit containing recombinant hnAChRs (alpha2beta4, alpha3beta4 and alpha4beta4) vs. beta2-subunit containing nAChRs (alpha4beta2 and alpha3beta2) both in terms of efficacy and potency[2].

[In Vivo]

SIB-1553A hydrochloride (1-40 mg/kg; s.c.) produces dose-dependent increases in ACh levels[3]. Animal Model: Male Sprague-Dawley rats (200-250 g)[3] Dosage: 1, 2, 4, 10, 20 and 40 mg/kg Administration: s.c. Result: Induced hippocampal ACh release.

[References]

[1]. Vernier JM, et al. 4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors. J Med Chem. 1999 May 20;42(10):1684-6.

[2]. Rao TS, et al. In vitro pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A), a nicotinic acetylcholine receptor ligand. Brain Res. 2003 Aug 15;981(1-2):85-98.

[3]. Rao TS, et al. In vivo pharmacological characterization of (+/-)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thiophenol hydrochloride (SIB-1553A), a novel cholinergic ligand: microdialysis studies. Brain Res. 2003 Oct 3;986(1-2):71-81.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₃H₂₀ClNOS

[ Molecular Weight ]:
273.822

[ Exact Mass ]:
273.095398

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.