Bethanechol chloride(氯贝胆碱) CH O NH2 Bethanechol chloride 2-[(Aminocarbonyloxy-NN, N-trimethyl-l-propanaminium chloride CH H2 H3C (S)-Bethanechol Chloride(R)-Bethanechol Chloride 240 fold
Bethanechol Chloride （氯贝胆碱） 2-[(Aminocarbonyl)oxy]-N,N,N-trimethyl-1-propanaminium chloride (S)-Bethanechol Chloride N O NH2 O H CH3 N O NH2 O H3C H (R)-Bethanechol Chloride > 240 fold
Actions and uses Potent muscarinic agonist. Orally effective, also administered by subcutaneous(皮下) Injection Increased hydrolytic stability(carbamate and steric bulk Stimulant of Gi tract smooth muscle and urinary bladder Uses: For the relief of post-surgical urinary retention (k 潴留) and abdominal distention(腹胀) Low toxicity, no serious side effects Should be used with caution in asthmatic(哮喘的) patients
Actions and Uses • Potent muscarinic agonist. Orally effective, also administered by subcutaneous(皮下) injection. • Increased hydrolytic stability (carbamate and steric bulk) • Stimulant of GI tract smooth muscle and urinary bladder. • Uses: For the relief of post-surgical urinary retention （尿 潴留） and abdominal distention （腹胀）. • Low toxicity, no serious side effects. • Should be used with caution in asthmatic （哮喘的） patients
Bethanechol chloride Synthesis OH COC\ O. CI NH3, EtoH Cl N(CH3)3
Bethanechol Chloride Synthesis:
Future Muscarinic Agonists Current research interest is focused on developing agents with selective affinity for muscarinic receptors in the brain. Potentially useful in the treatment of Alzheimer' s disease(阿尔茨海默尔) and other cognitive disorders.eg. Xanomeline(咕诺美林) Xanomeline
Future Muscarinic Agonists Current research interest is focused on developing agents with selective affinity for muscarinic receptors in the brain. Potentially useful in the treatment of Alzheimer’s disease （ 阿 尔 茨 海 默 尔 ） and other cognitive disorders. e.g. Xamomeline (呫诺美林)
3. 1.2 Acetylcholinesterase Inhibitors(AChEIs) Acetylcholinesterase(ache) AChE H3C-ON(CH3) H20 H3C OH HON(CH 3) Acetylcholine Inhibition of acetylcholinesterase (AChE) increases the concentration of acetylcholine (ACh) in the synapse. This results in prolonging the action of ACh, producing both muscarinic and nicotinic responses
3.1.2 Acetylcholinesterase Inhibitors (AChEIs) Acetylcholinesterase (AChE) Inhibition of acetylcholinesterase (AChE) increases the concentration of acetylcholine (ACh) in the synapse. This results in prolonging the action of ACh, producing both muscarinic and nicotinic responses