英国纽卡斯尔大学药理学课件11课程.pptVIP

Examples of muscarinic agonists and antagonists Clinical uses for muscarinic agonists and antagonists Drugs targeting nicotinic receptors Effect of nicotinic agonists and antagonists at neuromuscular junction Effect of nicotinic agonists and antagonists at neuromuscular junction Antagonist tubocurarine Hyperpolarisation, inhibition of EPPs Muscle fibre relaxation Paralysis Non-depolarising blocker Clinical uses for muscarinic and nicotinic agonists and antagonists Summary Clinical uses for muscarinic and nicotinic agonists and antagonists General mechanism ligand gated ion channel Synapse Postsynaptic cell body Cell membrane Neurotransmitter (e.g. ACh) ion channel ion (e.g. Na+, K+ ) ion Multiple cellular responses Ligand gated ion channels Structure: made up of 4 or 5 subunits structure Function: coupled directly to a ion channel Time scale: fast (milliseconds) Muscarinic receptors M1 M2 M3 G-protein coupled Slow response (seconds) Mainly located on effector tissues muscarine Cholinergic receptors Nicotinic receptor nic muscle, nic neurone Ligand gated ion channels Fast response (milliseconds) Located in ganglia and on NMJ nicotine Which functions/processes are mediated by which receptors? Mainly mediates parasympathetic effects Muscarinic receptors CNS Organ Ganglia Located at postganglionic parasympathetic synapses M Pupils constrict Lens of eye readjust for closer vision Airways in lungs constrict Heart rate decrease Blood vessels to limb muscles constrict Blood vessels to visceral organs more dilated Salivary secretions normalise Parasympathetic activation focal length of the lens (contraction of ciliary muscle) Effect of muscarinic agonists ? pupil constriction (contraction of constrictor pupillary muscle) Bronchoconstriction ?cardiac output, (rate force) GI motility exocrine gland secretion (sweating salivation, bronchiol secretion) Muscarinic agonists are known as parasympathomimetics Pupils constrict Lens of eye readjust