RECEPTORS

Shaik vaheeda rehman, Dept of pharmacology, 129A1SO605, Nimra college of pharmacy.

WHAT IS A RECEPTOR

RECEPTOR: It is a specific binding site on the cell which exhibits

some functional groups which trigger the pharmacological action

AFFINITY: Ability of agent to combine with receptor INTRINSIC ACTIVITY: Ability of agent to activate the receptor (efficacy) AGONIST: maximum affinity and efficacy ANTAGONIST: having affinity but no efficacy INVERSE AGONIST: having affinity and negative efficacy

Types of receptors: Iono tropic receptors

G-protein coupled receptors Enzymatic receptors Nuclear receptors

Ionotropic receptors:

G PROTEIN COUPLED RECEPTORS: General Structure of receptors:

Structure of G-protein:

G protein coupled with receptors:

Adenyl cyclase pathway:

Step by step mechanism of G protein coupling and enzyme activation

Phospholipase C pathway:

Second messengers:
cAMP system receptor 2,1,2 M2 Phosphoinositol system 1 M1,M3 Arachidonic acid system Histamine cGMP system Tyrosine kinase system

Transducer

Gs(1,2) Gq Gi(2, M2) AC Phospholipase C IP3,DAG

Unknown Gprotein Phospholipase A Arachidonic acid

Primary effector Secondary messenger Secondary effector

Guanylate Tyrosine cyclase kinase cGMP Protein phosphatase -

cAMP

Protein kinase A

Ca++ release

5-lipoxygenase Protein kinase G

Examples of G-protein receptors:

Muscarnic receptors (cholinergic) Adrenergic receptors (,) Histamine receptors Dopamine receptors Opiate receptors Serotonin receptors (all except 5-HT3) GABAB receptors

Enzymatic receptors:

Nuclear receptors:

Examples of nuclear receptors:

Glucocorticoid receptors Minero corticoid receptors Oestrogen receptors Progestero receptors Androgen receptors Vit A and vit B receptors Thyroid hormone receptors

Other receptors:
Normal receptors: Response observed when all the receptors of the
tissue occupied by drug moiety

Spare receptors: Maximum response is observed even though when all the
receptors of tissues are not occupied by drug moiety

Orphan receptors: Receptors with no endogenous ligand

Eg: PPAR- receptors (peroxysomal proliferated activated receptors)

Silent receptors: Biologically silent even though stimulations of receptors

taking place no biological response

REFERENCE: Pharmacology by RANG and DALE Integrated pharmacology by WALKER pharmacology by LIPPINCOTT pharmacology by BERTRUM www.wikkipedia.org www.winona.edu www.pharmacologycorner.com www.psychopharmacologyinstitute.com