A novel compound JPM8: in vivo penile activity promotion in rats, effect on the relaxation and cGMP/cAMP accumulation in isolated rabbit corpora cavernosa.
JPM8 is a novel sildenafil-like PDE5 inhibitor. Its efficacy was tested in vivo by the oral administration of drugs to a rat model and recording penile activity changes. Effect on the relaxation of the rabbit cavernosa was tested in vitro using an organ bath were drugs are added to the tissue media and relaxation was recorded using a transducer connected to a chart recorder. The accumulation of cGMP and cAMP was measured by incubation of cavernosa strips and then extracting the produced cGMP and cAMP in the incubation mixture, then quantitating it using ELISA. JPM8 showed increased and promoted sexual and penile activity in rats in a similar but slightly higher trend than the positive control sildenafil. JPM8 was more efficient in relaxing the rabbit corpora cavernosa than sildenafil. The cGMP and cAMP accumulation showed a similar trend for both drugs. We concluded that JPM8 was very effective in promoting sexual activity in rats, relaxing the corpora cavernosa and promoting cGMP accumulation in rabbits.
El-Thaher
T S
TS
The Jordanian Pharmaceutical Manufacturing Ltd, Naor Jordan.
Khatib
S
S
Saleem
M
M
Shnoudeh
A
A
Badwan
A A
AA
D015106:3',5'-Cyclic-GMP Phosphodiesterases; D000284:Administration, Oral; D000818:Animals; D000242:Cyclic AMP / Q000378:metabolism*; D006152:Cyclic GMP / Q000378:metabolism*; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D066298:In Vitro Techniques; D008297:Male; D009126:Muscle Relaxation; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D010410:Penile Erection / Q000187:drug effects*; D010413:Penis / Q000187:drug effects* / Q000502:physiology*; D010726:Phosphodiesterase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000187:drug effects*; D010879:Piperazines / Q000008:administration & dosage / Q000494:pharmacology*; D011687:Purines; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D000068677:Sildenafil Citrate; D013450:Sulfones
C475878:JPM8 compound; D010726:Phosphodiesterase Inhibitors; D010879:Piperazines; D011687:Purines; D013450:Sulfones; D000068677:Sildenafil Citrate; D000242:Cyclic AMP; D010727:Phosphoric Diester Hydrolases; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; C517384:Pde5a protein, rat; D006152:Cyclic GMP