作用于胆碱受体的药物（Drugs acting on cholinergic receptors）.docVIP

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作用于胆碱受体的药物（Drugs acting on cholinergic receptors）.doc

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作用于胆碱受体的药物（Drugs acting on cholinergic receptors）

作用于胆碱受体的药物（Drugs acting on cholinergic receptors） Drugs acting on cholinergic receptors 1. Cholinergic neurotransmitters and their receptors Transmitter: acetylcholine (acetilcholine, ACh) Synthesis, storage, release, and elimination of ACh 1) synthesis: ChAc Choline + AcCOA ACh 2) storage: vesicles; partly free form in cytoplasm 3) release: Quantum release: the amount of ACh released by each vesicle is a quantum A single nerve impulse can cause 200300 quantum release in the form of an extracellular cleft 4) eliminate Decomposition by acetylcholinesterase (Acetylcholinesterase, AchE): AchE Ach choline + acetic acid One molecule of AchE is hydrolyzed by 6 x 105 ACh molecules /min. Cholinergic receptor (Cholinergic Receptors), a receptor that can bind to ACh Nicotinic acetylcholine receptor Nicotinic Receptors receptor, N It is found in ganglion cell, adrenal medulla, chromaffin cell, neuromuscular junction, skeletal muscle, cell membrane and so on Two subtypes: NM (nicotinic, muscle) (N2) Located in the neuromuscular junction of the skeletal muscle cell membrane NN (nicotinic, neuronal) (N1) Located in the ganglion cell membrane, the central nervous system N cholinergic receptor: Ligand gated ion channel receptor 5 subunits: 2 alpha, beta, gamma, Delta The alpha subunit has a binding site for Ach Ach+ subunit subunit, ion channel opening to Na+, Ca2+, K+ ion flow Na+, Ca2+ goes into the cell and the muscles contract Synaptic vesicle Axon, ending, of, presynapic, cell Postsynapic cell Synaptic cleft Receptor for neurotransmitter Ions, that, affect, membrane, excitability Neurotransmitter, molecule, in, synaptic, cleft Receptor, for, the, neurotransmitter, on, postsynapic, cell Choline receptor, N, cholinergic receptor Present in the effector cell membrane of postganglionic cholinergic innervation MAchR (Muscarinic, Receptors, M receptor) Five subtypes: M1 gastric parietal cells, ganglia and central nervous cells M2, heart, etc M3 exocrine glands, smooth muscle, vascul