Title : (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.

Pub. Date : 1994 Jul

PMID : 7518514






3 Functional Relationships(s)
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1 ABT 418 was also approximately 10-fold less potent (EC50 value = 380 nM) than (-)-nicotine (40 nM) in increasing [3H]-dopamine release from rat striatal slices, an effect that was blocked by the nAChR antagonist, dihydro-beta-erythroidine (10 microM).2+ In contrast, ABT 418 appeared equipotent with (-)-nicotine in enhancing 86Rb+ flux from mouse thalamic synaptosomes. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus
2 However, a nAChR subtype selectivity may account for the in vitro potency differences of ABT 418 on various neurotransmitter systems, and the substantial separation between the cognitive enhancement/anxiolytic benefits, and the reduced central nervous system side-effect liabilities seen in vivo. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus
3 ABT 418 represents the first neuronal nAChR ligand that differentiates the toxicities/liabilities and other negative aspects normally associated with liabilities and other negative aspects normally associated with (-)-nicotine from the potential pharmacological benefits of selective cholinergic channel activation. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid cholinergic receptor nicotinic beta 1 subunit Rattus norvegicus