Silent alpha(2C)-adrenergic receptors enable cold-induced vasoconstriction in cutaneous arteries

Am J Physiol Heart Circ Physiol. 2000 Apr;278(4):H1075-83. doi: 10.1152/ajpheart.2000.278.4.H1075.

Abstract

Cold constricts cutaneous blood vessels by increasing the reactivity of smooth muscle alpha(2)-adrenergic receptors (alpha(2)-ARs). Experiments were performed to determine the role of alpha(2)-AR subtypes (alpha(2A)-, alpha(2B)-, alpha(2C)-ARs) in this response. Stimulation of alpha(1)-ARs by phenylephrine or alpha(2)-ARs by UK-14,304 caused constriction of isolated mouse tail arteries mounted in a pressurized myograph system. Compared with proximal arteries, distal arteries were more responsive to alpha(2)-AR activation but less responsive to activation of alpha(1)-ARs. Cold augmented constriction to alpha(2)-AR activation in distal arteries but did not affect the response to alpha(1)-AR stimulation or the level of myogenic tone. Western blot analysis demonstrated expression of alpha(2A)- and alpha(2C)-ARs in tail arteries: expression of alpha(2C)-ARs decreased in distal compared with proximal arteries, whereas expression of the glycosylated form of the alpha(2A)-AR increased in distal arteries. At 37 degrees C, alpha(2)-AR-induced vasoconstriction in distal arteries was inhibited by selective blockade of alpha(2A)-ARs (BRL-44408) but not by selective inhibition of alpha(2B)-ARs (ARC-239) or alpha(2C)-ARs (MK-912). In contrast, during cold exposure (28 degrees C), the augmented response to UK-14,304 was inhibited by the alpha(2C)-AR antagonist MK-912, which selectively abolished cold-induced amplification of the response. These experiments indicate that cold-induced amplification of alpha(2)-ARs is mediated by alpha(2C)-ARs that are normally silent in these cutaneous arteries. Blockade of alpha(2C)-ARs may prove an effective treatment for Raynaud's Phenomenon.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology
  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Arteries / chemistry
  • Arteries / physiology
  • Body Temperature Regulation / physiology
  • Brimonidine Tartrate
  • COS Cells
  • Cold Temperature*
  • Imidazoles / pharmacology
  • Indoles / pharmacology
  • Isoindoles
  • Isoquinolines / pharmacology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Microcirculation / physiology
  • Muscle, Smooth, Vascular / chemistry
  • Muscle, Smooth, Vascular / metabolism
  • Organ Culture Techniques
  • Phenylephrine / pharmacology
  • Piperazines / pharmacology
  • Quinolizines / pharmacology
  • Quinoxalines / pharmacology
  • Raynaud Disease / physiopathology
  • Receptors, Adrenergic, alpha-2 / metabolism*
  • Scleroderma, Systemic / physiopathology
  • Skin / blood supply*
  • Tail / blood supply
  • Vasoconstriction / drug effects
  • Vasoconstriction / physiology*

Substances

  • Adra2c protein, mouse
  • Adrenergic alpha-Agonists
  • Adrenergic alpha-Antagonists
  • Imidazoles
  • Indoles
  • Isoindoles
  • Isoquinolines
  • Piperazines
  • Quinolizines
  • Quinoxalines
  • Receptors, Adrenergic, alpha-2
  • L 657743
  • Phenylephrine
  • Brimonidine Tartrate
  • AR-C239
  • BRL 44408