Suven Life Sciences Ltd. has disclosed new 2-amino-pyrimidine derivatives acting as muscarinic M4 receptor positive allosteric modulators (PAMs) reported to be useful for the treatment of pain, sleep disorders, depression, schizophrenia, Alzheimer’s, Parkinson’s and Huntington’s disease.
Neurosterix Pharma Sarl has divulged 3-cyclopropylpyrazole derivatives acting as muscarinic M4 receptor positive allosteric modulators. They are reported to be useful for the treatment of psychiatric and neurological disorders.
Schizophrenia is a complex psychiatric disorder marked by positive, negative and cognitive symptoms, many of which are poorly addressed by current dopamine-blocking antipsychotics. Preclinical studies show that muscarinic acetylcholine M4 receptor positive allosteric modulators (M4 PAMs) can reduce hyperdopaminergic activity and improve both positive and negative symptom-related behaviors, suggesting they may offer enhanced antipsychotic efficacy with improved tolerability.
Positive allosteric modulators (PAMs) of the muscarinic acetylcholine M4 receptor show potential against schizophrenia because they can enhance endogenous acetylcholine signaling, which in turn may mitigate psychotic symptoms as well as improve attention and working memory in individuals with the disorder. However, the efficacy of a promising PAM, CVL-231, has been disappointing in clinical trials.
Dysregulation of cholinergic neurotransmission through muscarinic receptors, particularly the M1 and M4 subtypes, has been implicated in the pathophysiology of schizophrenia. Muscarinic M4 receptor agonists and positive allosteric modulators (PAMs) have demonstrated the ability to modulate the disrupted neural circuits associated with this disorder.
Vanderbilt University has synthesized muscarinic M4 receptor positive allosteric modulators (PAMs) reported to be useful for the treatment of Alzheimer’s disease, pain, schizophrenia and sleep disorders.
Muscarinic M4 receptor positive allosteric modulators are detailed in an Acadia Pharmaceuticals Inc. patent. They are reported to be useful for the treatment of Alzheimer’s disease, pain, schizophrenia, Huntington’s disease, Parkinson’s disease, psychosis and drug abuse and dependence.
Suven Life Sciences Ltd. has synthesized muscarinic M4 receptor positive allosteric modulators (PAMs) reported to be useful for the treatment of pain, psychiatric disorders and neurological disorders.
Researchers from China Pharmaceutical University and Jiangsu Nhwa Pharmaceutical Co. Ltd. have synthesized azetidine-containing compounds acting as muscarinic M4 receptor positive allosteric modulators (PAMs) reported to be useful for the treatment of Alzheimer’s disease, asthma, pain, schizophrenia, pulmonary hypertension, Huntington’s disease, Parkinson’s disease and sleep disorders among others.
