Polysorbate-80 surface modified nano-stearylamine BQCA conjugate for the management of Alzheimer's disease.

ABSTRACT: Acetylcholinesterase (AChE) inhibitors such as donepezil, galantamine and rivastigmine are used for the management of dementia in Alzheimer's Disease (AD). These drugs elevate endogenous acetylcholine (ACh) levels at the M₁ muscarinic receptor in the brain to achieve therapeutic benefits. However, their side effects, such as nausea, vomiting, dizziness, insomnia, loss of appetite, altered heart rate, etc., are related to non-specific peripheral activation of M₂-M₅ muscarinic subtypes. It is logical, therefore, to develop drugs that selectively activate brain M₁ receptors. Unfortunately, the orthosteric site homology among the receptor subtypes does not permit this approach. An alternative approach is to use positive allosteric modulator (P

SUBMITTER: Chintamaneni PK 

PROVIDER: S-EPMC8694636 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature