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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]
[object Object],[object Object],[object Object]
FEATURES – ION CHANNELS ,[object Object],[object Object],[object Object],[object Object]
MOLECULAR   STRUCTURE ,[object Object],[object Object],[object Object],[object Object]
Ligand binding site
 
 
 
 
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]
[object Object],[object Object],[object Object]
MOLECULAR STRUCTURE
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]
RHO A / RHO KINASE SYSTEM
[object Object],[object Object],[object Object],[object Object]
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
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
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
CLASS II
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]
 

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Drug receptors in pharmacology

  • 1.  
  • 2. Presented by P.Bindu, M.Pharmacy 1 st year, Department of Pharmacology, Sri padmavathi mahila viswavidyalayam, Tirupati.
  • 3.
  • 4.
  • 5.
  • 6.
  • 7.  
  • 8.
  • 9.  
  • 10.
  • 11.
  • 12.
  • 13.
  • 15.  
  • 16.  
  • 17.  
  • 18.  
  • 19. GATING MECHANISM IN GABA A RECEPTOR
  • 20.
  • 21.
  • 22.
  • 24.
  • 25.
  • 26.  
  • 27.  
  • 28.
  • 29. 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
  • 30.
  • 31.
  • 32.  
  • 33.
  • 34.  
  • 35.
  • 36. RHO A / RHO KINASE SYSTEM
  • 37.
  • 38. 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
  • 39.
  • 40. Kinase cascade Gene transcription
  • 41.
  • 42.
  • 43. Zn fingers;hor response elements -Binds with corepressor coactivator ptns AF 1 AF 2
  • 44.
  • 45. homo HRE- hormone response elements CLASS - I
  • 47. 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
  • 48.
  • 49.
  • 50.  

Notes de l'éditeur

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