PHA 4107 Lecture Notes - Lecture 8: Acetyl-Coa, Acetylcholine Receptor, Choline

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Synthesis of ach: choline is transported into the presynaptic cholinergic nerve terminal by a high affinity na+ choline co-transporter. The cytosolic enzyme choline acetyltansferase catalyzes the formation of acetylcholine (ach) from acetyl coenzyme a (accoa) and choline. Newly synthesized ach is packaged into vesicles for storage: released acetylcholine diffuses in the synaptic cleft and binds to postsynaptic and presynaptic receptors, acetylcholine in the synaptic cleft is degraded by membrane-bound acetylcholinesterase (ache) into choline and acetate. Cholinergic receptors: muscarine receptor, muscarine (agonist, atropine (antagonist, nicotine receptor, nicotine (agonist, tubocurarine* (antagonist, succinylcholine (depolarizing antagonist, hexamethonium (antagonist) Cns neurons, sympathetic postganglionic neurons, some presynaptic sites. Activation of the muscarainic receptors is often termed sludge: salivation, lacrimation, urination, defection, gastrointestinal motility, emesis (vomiting) Cholinergic drugs: cholinomimetics, direct acting, muscarinic agonists and nicotinic agonists, indirectly acting. Inhibitors of acetylcholinesterase: cholinolytics, muscarinic antagonists, autonomic ganglion inhibitors, neuromuscular relaxants, skeletal muscle nicotinic antagonist. Chewing the betel nut makes the saliva become red.

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