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Summary Medicinal chemistry of adrenergic neurones
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Neurophysiology, synaptic pharmacology and endocrinology - 1st semester Includes bullet points, key diagrams and images
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Medicinal Chemistry of Adrenergic ReceptorsAdrenergic Receptors
α and β- GPCRs
Signal transduction:
α1- generate IP3 and DAG
α2- inhibit generation of cAMP
β 1,2 and 3- generate cAMP
Biosynthesis of Adrenaline
Controlled by regulation of tyrosine hydroxylase
Inhibited by noradrenaline feedback
Adrenergic Binding site
, On TM5-Ser 207 and 204 (OHs) hydrogen bond acceptor for catechol OHs
On TM6-Phe 290 (arene) pi-pi stacking and Asn 293 hydrogen bond acceptor on
amide
TM3- Asp 113 (carboxylate) ionic with secondary amine
Metabolism
COMT
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