Vasodilator drugs

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Vasodilator drugs are drugs that produce vasodilation

Compounds may be grouped as endogenous and exogenous.

Endogenous

Vasodilators	Receptor (↑ = opens. ↓ = closes)	Transduction (↑ = increases. ↓ = decreases)
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 --> phosphorylation of MLCK --> ↓MLCK activity --> dephosphorylation of MLC open Ca2+-activated and voltage-gated K+channels --> hyperpolarization --> close VDCC --> ↓intracellular Ca2+
(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 --> ↓intracellular Na2+ --> ↑Na+/Ca2+ exchanger activity --> ↓intracellular Ca2+
Bradykinin	Bradykinin receptor
Substance P
Niacin (nicotinic acid)
Platelet activating factor (PAF)
CO2	-	↓interstitial pH --> ?
(probably) interstitial lactic acid	-
muscle work	-	↑vasodilators: ↑ATP consumption --> ↑adenosine ↑glucose usage --> CO2 ↑interstitial K+ ↑(extracellular) ATP ↑(extracellular) ADP ↑interstitial K+ ↓vasoconstrictors: ↑ATP consumption --> ↓ ATP (intracellular) ↓oxygen --> ↓oxidative phosphorylation --> ↓ ATP (intracellular)

Exogenous vasodilators

• Absence of high levels of environmental noise
• Absence of high levels of illumination
• Adenocard - Adenosine agonist, primarily used as an anti-arrhythmic.
• Alpha blockers (block the vasoconstricting effect of adrenaline).
• Amyl nitrite and other nitrites are often used recreationally as a vasodilator, causing lightheadedness and a euphoric feeling.
• Atrial natriuretic peptide (ANP) - a weak vasodilator.
• Ethanol
• Histamine-inducers
  • Complement proteins C3a, C4a and C5a work by triggering histamine release from mast cells and basophil granulocytes.
• Nitric oxide inducers
  • Glyceryl trinitrate (commonly known as Nitroglycerin)
  • Isosorbide mononitrate & Isosorbide dinitrate
  • Pentaerythritol Tetranitrate (PETN)
  • Sodium nitroprusside
  • PDE5 inhibitors: these agents indirectly increase the effects of nitric oxide
    • Sildenafil (Viagra)
    • Tadalafil
    • Vardenafil
• Tetrahydrocannabinol (THC) - the major active chemical in marijuana. Its mild vasodilating effects redden the eyes of cannabis smokers.
• Theobromine.
• Papaverine an alkaloid found in the opium poppy papaver somniferum

See also

• Antihypertensive drugs
• Blood pressure
• Channel blockers
• Heart rate effecting drugs
• Nicotinic acid
• Vasoconstrictor drugs
• Verapamil