Pharmacodynamic profile of fenoverine, a novel modulator of smooth muscle motility.
Experimental research has documented that fenoverine is a depressant drug mostly active on the intestinal smooth muscle; however, it is also active on other tissues as well as on the genito-urinary tract. Fenoverine may be considered a synchronizer of smooth muscle effective in modulating the intracellular influx of calcium into the cell and its release from the intracellular pool. Fenoverine causes a reduction of the excitatory junction potential (EJP) in intestinal smooth muscle by stimulating parasympathetic efferent fibres without any change in the inhibitory junction potential (IJP). This also occurs in the presence of atropine. Fenoverine reduces the intracellular Ca2+ concentration by decreasing the calcium gradient across the cell membrane, as well as decreasing the release of Ca2+ from the intestinal pool more intensely than papaverine (but less intensely than nifedipine, verapamil or diltiazem). This phenomenon has been observed in the intestinal smooth muscle and also in the genito-urinary tract.
De Santis
D
D
Institute of Pharmacology and Toxicology, 1st Faculty of Medicine and Surgery, University of Naples, Italy.
Marrazzo
R
R
Losasso
C
C
Loffreda
A
A
De Paola
C
C
De Novellis
V
V
Molinario
L
L
Schiariti
F
F
Marmo
E
E
D000818:Animals; D001285:Atropine / Q000494:pharmacology; D002415:Cats; D004576:Electromyography; D005260:Female; D005704:Gallbladder / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007422:Intestines / Q000187:drug effects; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects*; D010276:Parasympatholytics / Q000493:pharmacokinetics* / Q000494:pharmacology; D010640:Phenothiazines / Q000493:pharmacokinetics* / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D014132:Trachea / Q000187:drug effects; D001743:Urinary Bladder / Q000187:drug effects; D014599:Uterus / Q000187:drug effects; D010879:Piperazines
D001285:Atropine; D010276:Parasympatholytics; D010640:Phenothiazines; C048314:fenoverine; D010879:Piperazines