The neurovascular mechanism of clitoral erection: nitric oxide and cGMP-stimulated activation of BKCa channels

FASEB J. 2004 Sep;18(12):1382-91. doi: 10.1096/fj.04-1978com.

Abstract

Female sexual function is under-studied, and mechanisms of clitoral engorgement-relaxation are incompletely understood. Penile erection results from nitric oxide (NO) -induced cyclic guanosine monophosphate (cGMP) accumulation. cGMP-dependent protein kinase (PKG) activates large-conductance, calcium-activated potassium channels (BK(Ca)), thereby hyperpolarizing and relaxing vascular and trabecular smooth muscle cells, allowing engorgement. We hypothesize rat clitorises relax by a similar mechanism. Rat clitorises express components of the proposed pathway: neuronal and endothelial NO synthases, soluble guanylyl cyclase (sGC), type 5 phosphodiesterase (PDE-5), and BK(Ca) channels. The NO donor diethylamine NONOate (DEANO), the PKG activator 8-pCPT-cGMP, and the PDE-5 inhibitor sildenafil, cause dose-dependent clitoral relaxation that is inhibited by antagonists of PKG (Rp-8-Br-cGMPS) or BK(Ca) channels (iberiotoxin). Electrical field stimulation induces tetrodotoxin-sensitive NO release and relaxation that is inhibited by the Na+ channel blocker tetrodotoxin or sGC inhibitor 1H-(1,2,4)oxadiozolo(4,3-a)quinoxalin-1-one. Human BK(Ca) channels, transferred to Chinese hamster ovary cells via an adenoviral vector, and endogenous rat clitoral smooth muscle K+ current are activated by this PKG-dependent mechanism. Laser confocal microscopy reveals protein expression of BK(Ca) channels on clitoral smooth muscle cells; these cells exhibit BK(Ca) channel activity that is activated by both DEANO and sildenafil. We conclude that neurovascular derived NO causes clitoral relaxation via a PKG-dependent activation of BK(Ca) channels. The BK(Ca) channel is an appealing target for drug therapy of female erectile dysfunction.

Publication types

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

MeSH terms

  • Animals
  • CHO Cells
  • Calcium / metabolism
  • Clitoris / anatomy & histology
  • Clitoris / blood supply
  • Clitoris / innervation
  • Clitoris / physiology*
  • Cricetinae
  • Cyclic GMP / metabolism*
  • Cyclic GMP-Dependent Protein Kinases / metabolism
  • Electric Stimulation
  • Electrophysiology
  • Female
  • Humans
  • Immunohistochemistry
  • In Vitro Techniques
  • Large-Conductance Calcium-Activated Potassium Channels
  • Lasers
  • Microdissection
  • Muscle Relaxation / drug effects
  • Muscle, Smooth / blood supply
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / innervation
  • Muscle, Smooth / physiology
  • Nitric Oxide / biosynthesis
  • Nitric Oxide / metabolism*
  • Piperazines / pharmacology
  • Potassium Channels, Calcium-Activated / genetics
  • Potassium Channels, Calcium-Activated / metabolism*
  • Purines
  • Rats
  • Rats, Sprague-Dawley
  • Signal Transduction / drug effects
  • Sildenafil Citrate
  • Sulfones

Substances

  • Large-Conductance Calcium-Activated Potassium Channels
  • Piperazines
  • Potassium Channels, Calcium-Activated
  • Purines
  • Sulfones
  • Nitric Oxide
  • Sildenafil Citrate
  • Cyclic GMP-Dependent Protein Kinases
  • Cyclic GMP
  • Calcium