Milameline (CI-979, PD-129,409, RU-35,926) is a
non-selective muscarinic acetylcholine receptor
Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors that form G protein-coupled receptor, G protein-coupled receptor complexes in the cell membranes of certain neurons and other Cell (biology), cells. They play several role ...
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...
with
cognition
Cognition is the "mental action or process of acquiring knowledge and understanding through thought, experience, and the senses". It encompasses all aspects of intellectual functions and processes such as: perception, attention, thought, ...
-acting properties that was being investigated for the treatment of
Alzheimer's disease
Alzheimer's disease (AD) is a neurodegenerative disease and the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in remembering recent events. As the disease advances, symptoms can include problems wit ...
, but produced poor results in
clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s and was subsequently discontinued.
*Changing the ''O''-methyl aldoxime to an ''O''-
propargyl
In organic chemistry, the propargyl group is a functional group of 2- propynyl with the structure . It is an alkyl group derived from propyne ().
The term propargylic refers to a saturated position ( ''sp''3-hybridized) on a molecular framework ...
oxime instead gives a separate molecule called
RU 35986.
See also
*
Alvameline
*
Sabcomeline
*
Tazomeline
*
Xanomeline
Xanomeline (developmental code name LY-246,708) is a small molecule muscarinic acetylcholine receptor agonist that was synthesized in a collaboration between Eli Lilly and Novo Nordisk as an investigational therapeutic being studied for the tre ...
References
{{Muscarinic acetylcholine receptor modulators
Abandoned drugs
Aldoximes
M1 receptor agonists
M2 receptor agonists
M3 receptor agonists
M4 receptor agonists
M5 receptor agonists
Oxime ethers
Tetrahydropyridines