Drug receptors in pharmacology

Presented by P.Bindu, M.Pharmacy 1 st year, Department of Pharmacology, Sri padmavathi mahila viswavidyalayam, Tirupati.

CONTENTS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

WHAT IS A RECEPTOR? ,[object Object],[object Object],[object Object],[object Object]

DRUG RECEPTOR INTERACTIONS ,[object Object],[object Object],[object Object]

CONTD… ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

CONTD.. ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

RECEPTOR CLASSIFICATION - IUPHAR ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

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FEATURES – ION CHANNELS ,[object Object],[object Object],[object Object],[object Object]

MOLECULAR STRUCTURE ,[object Object],[object Object],[object Object],[object Object]

GATING MECHANISM IN GABA A RECEPTOR

CONTD . ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

ION CHANNELS - IMPORTANCE ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

FAMILIES OF GPCR ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

G-PROTEIN -ROLE ,[object Object],[object Object],[object Object],[object Object]

G-PROTEIN SUBTYPES G-PROTEIN RECEPTOR FOR SIGNALLING PATHWAY G S Beta adrenergic amines, glucagon histamine, serotonin ,[object Object],[object Object],[object Object],G i1, G i2 , G i3 Alpha 2 adrenergic amines, mAchR, opioid, serotonin adenylyl cyclase CAMP Cardiac K + channel open- heart rate G olf Olfactory epithelium Adenylyl cyclase – CAMP

G-PROTEIN RECEPTOR FOR SIGNALLING PATHWAY G O NT ,Opioid cannabinoid Not clear G q mAchR, serotonin 5HT 1C PLC IP 3 , DAG Cytoplasmic Ca G t1 , G t2 Rhodopsin and colour opsins in retinal rod and cone cells cGMP phosphodiesterase- cGMP

SECONDARY MESSENGER SYSTEMS INVOLVED IN SIGNAL TRANSDUCTION ,[object Object],[object Object],[object Object],[object Object]

ADENYLYL CYCLASE/ CAMP SYSTEM ,[object Object],[object Object],[object Object],[object Object]

PHOSPHOLIPASE C-INOSITOL SYSTEM ,[object Object],[object Object],[object Object]

ION CHANNELS ,[object Object]

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Structure of Kinases linked receptors Y Y Y Y Y Y Extracellular domain Binds to the ligand (growth factor) Trans membrane domain Intracellular domain Endogenous kinases bind and get phosphorlated

TYPES ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

Kinase cascade Gene transcription

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Zn fingers;hor response elements -Binds with corepressor coactivator ptns AF 1 AF 2

Class I Hybrid class Class II Present in cytoplasm Mainly endocrine Present in nucleus ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],High affinity binding Low affinity binding GR, MR, ER, PR, AR TR, VDR, RAR PPAR, LXR, FXR, RXR

homo HRE- hormone response elements CLASS - I

COMPARISON OF RECEPTORS TYPES INOTROPIC METABOTROPIC KINASE LINKED NUCLEAR NO.OF FAMILIES 483 217 135 48 LOCATION MEMBRANE MEMBRANE MEMBRANE INTRACELLULAR TIME SCALE MILLI SECONDS SECONDS HOURS HOURS COUPLING DIRECT VIA G-PROTIEN DIRECT VIA DNA EXAMPLES nAchR, GABA A ADRENOCEPTORS, mAchR INSULIN CYTOKINES GF STEROIDS

CONCLUSION ,[object Object],[object Object],[object Object],[object Object]

REFERENCES ,[object Object],[object Object],[object Object]

Drug receptors in pharmacology

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