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Vasodilator drugs

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Vasodilator drugs are drugs that produce vasodilation


Compounds may be grouped as endogenous and exogenous.

Endogenous

Vasodilators [1] Receptor
(↑ = opens. ↓ = closes) [1]
Transduction
(↑ = increases. ↓ = decreases) [1]
EDHF  ? hyperpolarization --> ↓VDCC --> ↓intracellular Ca2+
depolarization Voltage-gated K+ channel
interstitial K+ directly
nitric oxide NO receptor cGMP --> ↑PKG activity -->
  • phosphorylation of MLCK --> ↓MLCK activity --> dephosphorylation of MLC
  • SERCA --> ↓intracellular Ca2+
β2 adrenergic agonists β-2 adrenergic receptor Gs activity --> ↑AC activity --> ↑cAMP --> ↑PKA activity --> phosphorylation of MLCK --> ↓MLCK activity --> dephosphorylation of MLC
histamine Histamine H1 receptor
prostacyclin IP receptor
Prostaglandin D2 DP receptor
Prostaglandin E2 EP receptor
VIP VIP receptor Gs activity --> ↑AC activity --> ↑cAMP --> ↑PKA activity -->
(extracellular) adenosine A1, A2a and A2b adenosine receptors ATP-sensitive K+ channel --> hyperpolarization --> close VDCC --> ↓intracellular Ca2+
  • (extracellular) ATP
  • (extracellular) ADP
P2Y receptor activate Gq --> ↑PLC activity --> ↑intracellular Ca2+ --> ↑NOS activity --> ↑NO --> (see nitric oxide)
L-Arginine imidazoline and α-2 receptor? Gi --> ↓cAMP --> activation of Na+/K+-ATPase[2] --> ↓intracellular Na2+ --> ↑Na+/Ca2+ exchanger activity --> ↓intracellular Ca2+
Bradykinin Bradykinin receptor
Substance P
Niacin (nicotinic acid)
Platelet activating factor (PAF)
CO2 - interstitial pH --> ?[3]
(probably) interstitial lactic acid -
muscle work -

Exogenous vasodilators


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