3-Aminopropylphosphinic acid

Elebring etal, US Patent 6,576,626 (June 10, 2003) Assignee AstraZeneca AB 

Utility Treatment of Upper Gastrointestinal Tract Disorders 

Aminopropylphosphinic acids have also been prepared by reacting alkylphosphonite derivatives with propylene oxide followed by amination (1). 

The preparation of 3-methyl-3-hydroxy-3-(2-methylcyclohexyl)-2-(4-chloro-benzylamine)-propyl phosphinic acid, (I), is described (2). 

2-Oximinoalkylphosphonic acid esters have also been prepared (3). 

---

GABA is the predominant inhibitory neurotransmitter in the CNS. Baclofen acts centrally as an agonist at the GABAb receptor, which increases inhibition of nerves. 3-Aminopropylphosphinic acid (3-APPi) has been shown experimentally to act as an antitussive at peripheral nerves and preclinical evidence suggests that baclofen indeed has antitussive actions clinically [3]. 

GABA receptor agonists have been proposed as drugs for the treatment of bladder instability without side-effects on the central nervous system. 3-Aminopropylphosphinic acid (46, R, R R, R = H) inhibited the contraction of urinary bladder smooth muscle strips of rabbit by 45% when compared with controls. ... 

---