Investigating the role of protein kinase-G in the antidepressant-like response of sildenafil in combination with muscarinic acetylcholine receptor antagonism

Behav Brain Res. 2010 May 1;209(1):137-41. doi: 10.1016/j.bbr.2010.01.032. Epub 2010 Jan 29.

Abstract

The cGMP/PK-G pathway plays a crucial role in neuroprotection and neurotrophin support, and is possibly involved in antidepressant action. Recently we reported on a novel antidepressant-like response following simultaneous administration of sildenafil (phosphodiesterase 5 (PDE5) inhibitor, thereby increasing cGMP levels), and atropine (muscarinic acetylcholine receptor antagonist) in the rat forced swim test (FST). However, it is unclear whether the antidepressant-like activity of sildenafil+atropine is mediated via the activation of PK-G, an important down-stream effector for cGMP, and whether this may target known pathways in antidepressant action. We investigated whether the antidepressant-like response of sildenafil+/-atropine could be reversed by Rp-8-Br-PET-cGMP, a PK-G inhibitor, and also whether a combination of 8-Br-cGMP (PK-G activator)+/-atropine would likewise be active in the FST, and whether this combination could be attenuated by a PK-G inhibitor. 8-Br-cGMP alone, but not sildenafil alone, reduced immobility and selectively increased swimming in the FST. The antidepressant-like action of sildenafil was only evident following co-administration of atropine, and selectively increased climbing behaviour. Importantly, PK-G inhibition prevented the antidepressant-like effects of both 8-Br-cGMP and the sildenafil/atropine combination. These results confirm cholinergic-cGMP-PK-G interactions in the antidepressant-like effects of sildenafil, putatively acting via noradrenergic mechanisms, whereas direct PK-G activation induces antidepressant-like effects that are associated with enhancement of serotonergic neurotransmission.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Atropine / pharmacology*
  • Atropine / therapeutic use
  • Behavior, Animal / drug effects
  • Cyclic GMP / analogs & derivatives
  • Cyclic GMP / metabolism
  • Cyclic GMP / pharmacology
  • Cyclic GMP-Dependent Protein Kinases / metabolism*
  • Depression / drug therapy*
  • Depression / physiopathology
  • Disease Models, Animal
  • Drug Administration Routes
  • Drug Interactions / physiology
  • Drug Therapy, Combination
  • Freezing Reaction, Cataleptic / drug effects
  • Male
  • Muscarinic Antagonists / pharmacology*
  • Phosphodiesterase Inhibitors / pharmacology*
  • Phosphodiesterase Inhibitors / therapeutic use
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Purines / pharmacology
  • Purines / therapeutic use
  • Rats
  • Rats, Sprague-Dawley
  • Sildenafil Citrate
  • Statistics, Nonparametric
  • Sulfones / pharmacology*
  • Sulfones / therapeutic use
  • Swimming / psychology
  • Thionucleotides / pharmacology

Substances

  • Muscarinic Antagonists
  • Phosphodiesterase Inhibitors
  • Piperazines
  • Purines
  • Sulfones
  • Thionucleotides
  • 8-bromoguanosino-3',5'-cyclic monophosphorothioate
  • 8-bromo-beta-phenyl-1,N(2)-ethenoguanosine 3',5'-cyclic monophosphorothioate
  • Atropine
  • Sildenafil Citrate
  • Cyclic GMP-Dependent Protein Kinases
  • Cyclic GMP