PHAR2210 Lecture Notes - Lecture 8: Nicotinic Acetylcholine Receptor, Adenylyl Cyclase, Insulin Receptor

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Receptors superfamilies: receptors sub-divided into 4 major types or superfamilies: Ligand-gated ion channel receptors: g protein-coupled receptors, enzyme-linked receptors, nuclear receptors. Located in the cell membrane: are usually collections of proteins forming a central pore (channel, no agonist, ion channel closed, no ion flow. Ions cannot cross cell membrane: acetylcholine (ach) binding alters ion channel structure and ions flow into the cell. Effector: channel located in the membrane: respond to: fast neurotransmitters. Pancuronium, a nicotinic acetylcholine receptor antagonist, is used to produce paralysis during anaesthesia. Effector: enzyme or channel: respond to: hormones, slow neurotransmitters. Salbutamol, a 2- adrenoceptor agonist, relieves bronchospasm in asthma: g proteins: intracellular effector systems or 2nd messenger cascades, guanosine nucleotide binding proteins, gtp and gdp, comprises 3 subunits ( , , ) Effector: enzyme location is in membrane: respond to: metabolism, growth, differentiation. Examples: insulin receptor, receptors for cytokines, growth factors. In diabetes, insulin is used to activate the insulin receptor and reduce blood glucose levels.

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