ADRENERGIC RECEPTOR AGONIST AND ANTAGONIST Flashcards
What do adrenoreceptors do
Adrenoceptors mediate central and peripheral actions of NA (NT) & Adr. (hormone & NT).
Where are adrenoceptors found
Found in nearly all peripheral tissues & on many neuronal populations within the CNS.
Functions of adrenoceptos agonist and antagonist
Agonists & antagonists have proved useful in treatment of variety of diseases including hypertension, angina pectoris, CHF, asthma, depression, BPH & glaucoma.
Also useful in therapeutic situations e.g. shock, premature labour, opioid withdrawal & as adjuncts to general anaesthesia.
AJA
What are the types of adrenoreceptors
α , β
α1, α2
β1 , β2 , β3 , β4
α2A , α2B , α2C , (α2D)
α1A , α1B , α1D , (α1L)
What is α2D
α2D is a species orthologue of the human α2A subtype hence it is not considered to be a separate subtype
What is α1L
α1L may represent a particular conformational state of the α1A-ADR.
What tissues are alpha1 receptors found and what’s the effect
• Most vascular smooth muscle ;contract (vascular resistance)
• Pupillary dilator muscle ; contract (mydriasis)
• Pilomotor smooth muscle ; contract (erects hair)
What tissues are alpha 2 receptors found and their effect
Adrenergic and cholinergic nerve terminals (inhibit transmitter release)
Platelets
Some vascular smooth muscle
What’s the distribution of the adrenergic receptors
Alpha 1: almost all effectors
Alpha 2: preganglionic neuron
Beta 1: heart
Beta 2: almost all effectors
Beta 3: adipocytes
What are the distribution of the adrenergic receptors
Alpha 1: Gq
Alpha 2: Gi
Beta 1-3: Gs
What adrenergic receptor controls the eyes and it’s effect
Alpha1, beta 2
Myadriasis (pupillary dilatation)
What adrenergic receptor controls the salivary gland and it’s effect
Alpha 1, beta 2
Thick mucus saliva
What adrenergic receptor controls the lungs and it’s effect
Beta 2
Bronchodialtion
What adrenergic receptor affects the heart and it’s effect
Beta 1
Increased HR and FC
What adrenergic receptor affects the GIT and it’s effect
Alpha 1 Beta 2
Reduced motility and increased feacal retention