In vitro pharmacological characterization of (±)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A), a nicotinic acetylcholine receptor ligand

• Published in: Brain research Vol. 981; no. 1; pp. 85 - 98
• Main Authors: Rao, Tadimeti S., Adams, Pamala B., Correa, Lucia D., Santori, Emily M., Sacaan, Aida I., Reid, Richard T., Suto, Carla M., Michel Vernier, Jean
• Format: Journal Article
• Language: English
• Published: London Elsevier B.V 15.08.2003; Amsterdam Elsevier; New York, NY
• Subjects: Animals; Attention - drug effects; Biological and medical sciences; Brain - anatomy & histology; Brain - metabolism; Calcium - metabolism; Cell Line - metabolism; Cholinergic system; Cholinesterase Inhibitors; Cholinesterases - blood; Cognition - drug effects; Dopamine Uptake Inhibitors - pharmacology; Dose-Response Relationship, Drug; Drug Interactions; Embryo, Mammalian; Extracellular Space - metabolism; Humans; In Vitro Techniques; Ligands; Male; Medical sciences; N-Methylaspartate - pharmacology; Neuropharmacology; Neurotransmitter Agents - metabolism; Neurotransmitters. Neurotransmission. Receptors; Nicotinic acetylcholine receptor; Nicotinic Agonists - pharmacology; Nicotinic Antagonists - pharmacokinetics; Nomifensine - pharmacology; Pharmacology. Drug treatments; Phenols - pharmacology; Physostigmine - pharmacology; Protein Subunits - metabolism; Pyrrolidines - pharmacology; Radioligand Assay - methods; Rats; Rats, Sprague-Dawley; Receptors, Nicotinic - metabolism; Recombinant Proteins - metabolism; SIB-1553A; SIB-1553A; Neurotransmitters, modulators, transporters and receptors; Nicotinic acetylcholine receptor; Characterization; Cholinergic receptor; Ligand; Nicotinic receptor

SIB-1553A ((±)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol HCl) is a neuronal nicotinic acetylcholine receptor (nAChR) ligand which displaced the binding of [ 3H]nicotine (NIC) to the rat brain nAChRs with an IC 50 value of 110 nM with no appreciable affinity to the α7 nAhRs. SIB-1553A showed mo...