1. Adrenergic Drugs II Aims To understand the actions and side effects of major adrenergic drugs, and their clinical applications Read: Chapter 8, Rang and Dale comments to Dr Ian Musgrave (336S) Email: Ian.Musgrave@adelaide.edu.au
8. Close up of Adrenergic terminal NA NA NA NA Tyrosine Dopamine DOPA NA MAO NA NA Metabolites Uptake 1 Vesicular transporter TH DDC D H Vesicular transporter Cocaine
15. Effect of tolazoline and phenoxybenzamine on noradrenergic contraction in cat splenic strips + Tolazoline + Phenoxybenzamine Competitive vs non-competitive antagonism
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18. Adrenaline “reversal” adrenaline adrenaline Prazosin Blood Presure Blockade of vasoconstrictor 1 -adrenoceptors reveals vasodilator -adrenoceptors Time Time Blood pressure recordings in anaesthetised dog
24. Adrenaline with and without propranolol adrenaline adrenaline propranolol Blodd Pressure Blockade of vasodilator -adrenoceptors reveals vasoconstrictor -adrenoceptors Time Time
33. Cartoon of adrenergic receptors showing the 7 transmembrane spanning domains G S Family G i/o Family Adenylyl cyclase +ve -ve ATP cAMP -adrenoceptors 2 -adrenoceptors Biological response cAMP dependent protein kinase
34. Structure-activity relationships Looking down on the -adrenoceptor from outside the membrane with adrenaline in the binding site between transmembrane domains 3,5 and 6 (model based on rhodopsin crystal structure) TM3 TM5 TM6
38. Indirect sympatholytics NA NA NA MeNA Tyrosine Dopamine DOPA NA NA NA Uptake 1 Vesicular transporter TH DDC D H Reserpine -ve Guanethidine -ve MethylDOPA -Methyl tyrosine -ve