altinicline

Altinicline (SIB-1508Y) is a **small molecule**, subtype-selective **neuronal nicotinic acetylcholine receptor (nAChR) agonist**, primarily targeting muscle-type and α4β2 nicotinic acetylcholine receptors. It was developed for neurological and neurodegenerative conditions, notably investigated for **Parkinson's disease**, as well as cognitive disorders. In preclinical models, it demonstrated behavioral effects such as increased dopamine release (primarily in striatum, nucleus accumbens, and prefrontal cortex), mild antiparkinsonian effects (potentiated when combined with levodopa), and improved cognitive function. However, clinical trials in humans showed limited efficacy and were associated with adverse effects like lightheadedness and emesis, leading to discontinuation of the drug's development after phase 2. The originator is Merck & Co., Inc., with prior development involvement also from SIBIA Neurosciences and Meiji Seika Pharma.

Other names

(S)-(2)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine HClaltinicline maleate