On Benzofuroindole Analogues as Smooth Muscle Relaxants

On Benzofuroindole Analogues as Smooth Muscle Relaxants

At least two laboratories have independently reported the synthesis of benzofuroindole compounds having potential therapeutic implications in many disease states including those that involve smooth muscle hyperactivity. Through a series of in vitro screenings, they demonstrated the efficacy (and selectivity) of these compounds to potentiate large conductance calcium- (Ca²⁺-) activated K⁺ (BK(Ca...

Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants.

In addition to its emerging immunodulatory properties, theophylline is a bronchodilator and also decreases mean pulmonary arterial pressure in vivo. The mechanism of action of this drug remains controversial; adenosine antagonism, phosphodiesterase (PDE) inhibition and other actions have been advanced to explain its effectiveness in asthma. Cyclic adenosine monophosphate (AMP) and cyclic guanos...

Use of muscle relaxants.

Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro.

Neuromuscular blocking drugs (NMBD) can inhibit not only nicotinic but also muscarinic (M) receptors and thereby affect not only skeletal but also smooth muscle (SM) tone. A selective postjunctional muscarinic inhibition would relax, while prejunctional inhibition of muscarinic M2 receptor might hasten SM contraction thereby increasing the risk of bronchospasm. In rat tracheal rings in vitro we...

Muscle relaxants and antispasticity agents.

Muscle relaxants make up a heterogeneous group of agents and can have a clinically significant role in the treatment of chronic muscle pain. These medications are not without possible serious side effects; hence, care should be taken in deciding on their appropriateness and ongoing monitoring performed, if prescribed.