abt-594 and Neuroblastoma

abt-594 has been researched along with Neuroblastoma* in 1 studies

Other Studies

1 other study(ies) available for abt-594 and Neuroblastoma

Article	Year
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors. Journal of medicinal chemistry, 1998, Feb-12, Volume: 41, Issue:4 New members of a previously reported series of 3-pyridyl ether compounds are disclosed as novel, potent analgesic agents acting through neuronal nicotinic acetylcholine receptors. Both (R)-2-chloro-5-(2-azetidinylmethoxy)pyridine (ABT-594, 5) and its S-enantiomer (4) show potent analgesic activity in the mouse hot-plate assay following either intraperitoneal (i.p.) or oral (p.o.) administration, as well as activity in the mouse abdominal constriction (writhing) assay, a model of persistent pain. Compared to the S-enantiomer and to the prototypical potent nicotinic analgesic agent (+/-)-epibatidine, 5 shows diminished activity in models of peripheral side effects. Structure-activity studies of analogues related to 4 and 5 suggest that the N-unsubstituted azetidine moiety and the 2-chloro substituent on the pyridine ring are important contributors to potent analgesic activity. Topics: Administration, Oral; Analgesics, Non-Narcotic; Animals; Azetidines; Diastole; Female; Humans; Injections, Intraperitoneal; Kinetics; Mice; Molecular Structure; Muscle Contraction; Neuroblastoma; Neurons; Nicotinic Agonists; Oocytes; Pain; Pain Measurement; Pyridines; Rats; Receptors, Nicotinic; Recombinant Proteins; Stereoisomerism; Structure-Activity Relationship; Tumor Cells, Cultured; Xenopus	1998

Article

Year

Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.

Journal of medicinal chemistry, 1998, Feb-12, Volume: 41, Issue:4

New members of a previously reported series of 3-pyridyl ether compounds are disclosed as novel, potent analgesic agents acting through neuronal nicotinic acetylcholine receptors. Both (R)-2-chloro-5-(2-azetidinylmethoxy)pyridine (ABT-594, 5) and its S-enantiomer (4) show potent analgesic activity in the mouse hot-plate assay following either intraperitoneal (i.p.) or oral (p.o.) administration, as well as activity in the mouse abdominal constriction (writhing) assay, a model of persistent pain. Compared to the S-enantiomer and to the prototypical potent nicotinic analgesic agent (+/-)-epibatidine, 5 shows diminished activity in models of peripheral side effects. Structure-activity studies of analogues related to 4 and 5 suggest that the N-unsubstituted azetidine moiety and the 2-chloro substituent on the pyridine ring are important contributors to potent analgesic activity.

Topics: Administration, Oral; Analgesics, Non-Narcotic; Animals; Azetidines; Diastole; Female; Humans; Injections, Intraperitoneal; Kinetics; Mice; Molecular Structure; Muscle Contraction; Neuroblastoma; Neurons; Nicotinic Agonists; Oocytes; Pain; Pain Measurement; Pyridines; Rats; Receptors, Nicotinic; Recombinant Proteins; Stereoisomerism; Structure-Activity Relationship; Tumor Cells, Cultured; Xenopus

1998