Literature summary for 3.1.4.35 extracted from

Filippi, S.; Morelli, A.; Sandner, P.; Fibbi, B.; Mancina, R.; Marini, M.; Gacci, M.; Vignozzi, L.; Vannelli, G.B.; Carini, M.; Forti, G.; Maggi, M.
Characterization and functional role of androgen-dependent PDE5 activity in the bladder (2007), Endocrinology, 148, 1019-1029.

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Application

Application	Comment	Organism
medicine	by blocking isoform PDE5, vardenafil may be used in bladder dysfunction by ameliorating irritative lower urinary tract symptoms	Rattus norvegicus

Inhibitors

Inhibitors	Comment	Organism	Structure
Cilostamide	-	Homo sapiens
Cilostamide	-	Rattus norvegicus
dipyridamole	-	Homo sapiens
dipyridamole	-	Rattus norvegicus
sildenafil	blocking of 70% of total cGMP hydrolizing activity	Homo sapiens
sildenafil	blocking of 70% of total cGMP hydrolizing activity	Rattus norvegicus
tadalafil	blocking of 70% of total cGMP hydrolizing activity	Homo sapiens
tadalafil	blocking of 70% of total cGMP hydrolizing activity	Rattus norvegicus
vardenafil	blocking of 70% of total cGMP hydrolizing activity. Blocking of enzyme with vardenafil increases the antiproliferative and relaxant effect of sodium nitroprusside on cells, which is almost ineffective in presence of active enzyme	Homo sapiens
vardenafil	blocking of 70% of total cGMP hydrolizing activity. Blocking of enzyme with vardenafil increases the antiproliferative and relaxant effect of sodium nitroprusside on cells, which is almost ineffective in presence of active enzyme	Rattus norvegicus
zaprinast	-	Homo sapiens
zaprinast	-	Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Rattus norvegicus	isoform PDE5 regulates bladder smooth muscle tone, strongly limiting the nitric oxide/cGMP signaling	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	isoform PDE5	-
Rattus norvegicus	-	isoform PDE5	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
bladder	vascular endothelium and muscle fibers	Homo sapiens	-
bladder	vascular endothelium and muscle fibers, castration decreases and T supplementation restores PDE5 gene expression	Rattus norvegicus	-
muscle	muscle fibers of bladder	Homo sapiens	-
muscle	muscle fibers of bladder	Rattus norvegicus	-
vascular endothelium	-	Homo sapiens	-
vascular endothelium	-	Rattus norvegicus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	isoform PDE5 regulates bladder smooth muscle tone, strongly limiting the nitric oxide/cGMP signaling	Rattus norvegicus	?	-	?

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000003	-	bladder homogenate, 30°C, pH 7.0	Homo sapiens	vardenafil
0.0000032	-	bladder homogenate, 30°C, pH 7.0	Homo sapiens	sildenafil
0.00000607	-	bladder homogenate, 30°C, pH 7.0	Homo sapiens	tadalafil
0.0000088	-	bladder homogenate, 30°C, pH 7.0	Homo sapiens	zaprinast
0.0000109	-	bladder homogenate, 30°C, pH 7.0	Homo sapiens	dipyridamole
0.0000405	-	bladder homogenate, 30°C, pH 7.0	Homo sapiens	Cilostamide

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Release 2023.1 (January 2023)