abt-594 and Pain

abt-594 has been researched along with Pain* in 2 studies

Other Studies

2 other study(ies) available for abt-594 and Pain

Article	Year
3-(2,5-Dihydro-1H-pyrrol-2-ylmethoxy)pyridines: synthesis and analgesic activity. Bioorganic & medicinal chemistry letters, 2005, Mar-15, Volume: 15, Issue:6 We disclose an efficient procedure for the preparation of ethers of 2-substituted 2-hydroxymethylpyrroline and of 2-aminomethyl-3-pyrrolines, involving, as a key step, formation and nucleophilic ring opening of a cyclic sulfamidate. Several new analogs of epibatidine (1) and tebanicline (ABT-594, 2) were prepared and tested for analgesic activity in the mouse formalin model. Topics: Analgesics, Non-Narcotic; Animals; Azetidines; Bridged Bicyclo Compounds, Heterocyclic; Mice; Models, Chemical; Molecular Structure; Pain; Pyridines	2005
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

3-(2,5-Dihydro-1H-pyrrol-2-ylmethoxy)pyridines: synthesis and analgesic activity.

Bioorganic & medicinal chemistry letters, 2005, Mar-15, Volume: 15, Issue:6

We disclose an efficient procedure for the preparation of ethers of 2-substituted 2-hydroxymethylpyrroline and of 2-aminomethyl-3-pyrrolines, involving, as a key step, formation and nucleophilic ring opening of a cyclic sulfamidate. Several new analogs of epibatidine (1) and tebanicline (ABT-594, 2) were prepared and tested for analgesic activity in the mouse formalin model.

Topics: Analgesics, Non-Narcotic; Animals; Azetidines; Bridged Bicyclo Compounds, Heterocyclic; Mice; Models, Chemical; Molecular Structure; Pain; Pyridines

2005

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