LY2033298 is a positive allosteric modulator of muscarinic M4 receptor.
LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 potentiates ACh-M4 binding, with no effect at M1/3/5 receptors. LY2033298 can also bind to the M ACh receptor, and mediate either positive or negative allosteric effects depending on the ligand used to probe receptor activity.
Características e benefícios
This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Proceedings of the National Academy of Sciences of the United States of America, 105(31), 10978-10983 (2008-08-06)
Current antipsychotics provide symptomatic relief for patients suffering from schizophrenia and related psychoses; however, their effectiveness is variable and many patients discontinue treatment due to side effects. Although the etiology of schizophrenia is still unclear, a leading hypothesis implicates an
The M4 muscarinic acetylcholine (ACh) receptor (mAChR) is a potential therapeutic target but characterized by a lack of subtype-selective ligands. We recently generated "designer receptors exclusively activated by a designer drug" (DREADDs), which contained mutations of two conserved orthosteric-site residues
Muscarinic acetylcholine receptors (mAChRs) provide viable targets for the treatment of multiple central nervous system disorders. We have used cheminformatics and medicinal chemistry to develop new, highly selective M4 allosteric potentiators. VU10010, the lead compound, potentiates the M4 response to
European journal of pharmacology, 882, 173274-173274 (2020-06-14)
Opioids strongly inhibit GABAergic neurons in the rostromedial tegmental nucleus (RMTg) that expresses μ-opioid receptors to induce rewarding and psychomotor effects. M3 and M4 muscarinic receptors are co-localized with μ-opioid receptors at these GABAergic neurons. This study explored whether RMTg
ACS chemical neuroscience, 5(10), 920-942 (2014-08-20)
Positive allosteric modulators (PAMs) of the M4 muscarinic acetylcholine receptor (mAChR) represent a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neuropsychiatric disorders. We recently reported that the selective M4 PAM VU0152100 produced an antipsychotic
Nossa equipe de cientistas tem experiência em todas as áreas de pesquisa, incluindo Life Sciences, ciência de materiais, síntese química, cromatografia, química analítica e muitas outras.
