Title : ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties.

Pub. Date : 1997 Oct

PMID : 9336329






3 Functional Relationships(s)
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1 In radioligand binding studies, ABT-089 was shown to display selectivity toward the high-affinity (-)-cytisine binding site present on the alpha4beta2 nAChR subtype (Ki = 16 nM) relative to the [125I]alpha-bungarotoxin binding site present on the alpha7 (Ki > or = 10,000 nM) and alpha1beta1deltagamma (Ki > 1000 nM) nAChR subtypes. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid cholinergic receptor nicotinic alpha 4 subunit Homo sapiens
2 In radioligand binding studies, ABT-089 was shown to display selectivity toward the high-affinity (-)-cytisine binding site present on the alpha4beta2 nAChR subtype (Ki = 16 nM) relative to the [125I]alpha-bungarotoxin binding site present on the alpha7 (Ki > or = 10,000 nM) and alpha1beta1deltagamma (Ki > 1000 nM) nAChR subtypes. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid cholinergic receptor nicotinic alpha 4 subunit Homo sapiens
3 The differential full agonist/partial agonist profile of ABT-089, as compared with (-)-nicotine and ABT-418, illustrates the complexity of nAChR activation and the potential to target responses at subclasses of the neuronal and peripheral receptors. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid cholinergic receptor nicotinic alpha 4 subunit Homo sapiens