ml253 and Schizophrenia

ml253 has been researched along with Schizophrenia* in 1 studies

Other Studies

1 other study(ies) available for ml253 and Schizophrenia

Article	Year
Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorganic & medicinal chemistry letters, 2013, Jan-01, Volume: 23, Issue:1 Herein we report a next generation muscarinic receptor 4 (M(4)) positive allosteric modulator (PAM), ML253 which exhibits nanomolar activity at both the human (EC(50)=56 nM) and rat (EC(50)=176 nM) receptors and excellent efficacy by the left-ward shift of the ACh concentration response curve (fold shift, human=106; rat=50). In addition, ML253 is selective against the four other muscarinic subtypes, displays excellent CNS exposure and is active in an amphetamine-induced hyperlocomotion assay. Topics: Allosteric Regulation; Amides; Animals; Brain; Cholinergic Agents; Disease Models, Animal; Drug Evaluation, Preclinical; Half-Life; Humans; Protein Binding; Pyridines; Rats; Receptor, Muscarinic M4; Schizophrenia; Structure-Activity Relationship; Thiophenes	2013

Article

Year

Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.

Bioorganic & medicinal chemistry letters, 2013, Jan-01, Volume: 23, Issue:1

Herein we report a next generation muscarinic receptor 4 (M(4)) positive allosteric modulator (PAM), ML253 which exhibits nanomolar activity at both the human (EC(50)=56 nM) and rat (EC(50)=176 nM) receptors and excellent efficacy by the left-ward shift of the ACh concentration response curve (fold shift, human=106; rat=50). In addition, ML253 is selective against the four other muscarinic subtypes, displays excellent CNS exposure and is active in an amphetamine-induced hyperlocomotion assay.

Topics: Allosteric Regulation; Amides; Animals; Brain; Cholinergic Agents; Disease Models, Animal; Drug Evaluation, Preclinical; Half-Life; Humans; Protein Binding; Pyridines; Rats; Receptor, Muscarinic M4; Schizophrenia; Structure-Activity Relationship; Thiophenes

2013