SYMPATHETIC RECEPTORS
INTRODUCTION:
- Adrenergic receptors/adrenoceptors/Sympathetic receptors – Class of G protein-coupled receptors.
- Targets catecholamines, mainly norepinephrine (noradrenaline) & epinephrine (adrenaline).
- Cells binds to catecholamine receptors & stimulates sympathetic nervous system.
- Sympathetic nervous system –
- Responsible for fight-or-flight response, including pupil diltation, increasing heart rate, mobilizing energy, & blood-flow divertion from non-essential organs to skeletal muscle.
RECEPTOR TYPES:
- α receptors:
- Subtypes
- α1 (a Gq coupled receptor)
- α2 (a Gi coupled receptor)
- Phenylephrine – Selective α-receptor agonist.
- β receptors:
- Subtypes:
- β1, β2 and β3.
- All three linked to Gs proteins (although β2 also couples to Gi & to adenylate cyclase.
- Agonist binding causes raised intracellular second messenger cAMP concentration.
- Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates intracellular events following hormone binding.
- Isoprenaline – non-selective agonist.

| Receptor | Location | Selected action | Mechanism | Agonist | Antagonist |
| α1 |
Vascular , GU smooth muscle
Liver Intestinal Smooth muscle Heart |
|
Gq:
phospholipase C(PLC) activated, IP3,and DAG, ↑ calcium |
|
(TCAs)
Antihistamines (H1 antagonists)
|
| α2 |
β-cell of pancreas
Platelet Nerve Terminal Vascular smooth muscle |
|
Gi:
adenylate cyclase inactivated, cAMP↓ |
|
|
| β1 |
Juxtraglomular cell
Heart |
|
Gs:
adenylate cyclase activated, cAMP↑ |
|
|
| β2 |
Smooth muscle (GI,GU,Vascular,Braonchial)
Skeletal Muscle |
|
Gs:
adenylate cyclase activated, cAMP↑ |
|
|
| β3 | Adipose Tissue |
|
Gs:
adenylate cyclase activated, cAMP↑ |
|
|
Exam Important
- Adreneric β receptors having lipolysis property in fat cells is Beta -3.
- Alpha 2 agonist cause analgesia & not hyperalgesia.
- Salmeterol is long acting beta-2-agonist.
- Beta-2-agonist causes a brief spell of hyperkalemia followed by hypokalemia.
- Beta-2-agonist doesn’t cause hypoglycemia.
- Alpha-2-agonist causes Sedation, Glaucoma & Hypertension.
- Beta-1 receptors in heart stimulates its contractions.
- Beta-2 receptors are present in smooth muscles.
- Beta-1 receptors stimulation releases renin.
- Beta blockers are used to treat hyperthyroidism (Not hypothyroidism).
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