Protein Information

Name PDE3
Synonyms CGI PDE A; CGI PDE; Cyclic GMP inhibited phosphodiesterase A; PDE3; PDE3A; cAMP phosphodiesterase 3; cAMP phosphodiesterase myocardinal cGMP inhibited; Cyclic GMP inhibited phosphodiesterase As…

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
12072589 Bardou M, Goirand F, Bernard A, Guerard P, Gatinet M, Devillier P, Dumas JP, Morcillo EJ, Rochette L, Dumas M: Relaxant effects of selective phosphodiesterase inhibitors on U46619 precontracted human intralobar pulmonary arteries and role of potassium channels. J Cardiovasc Pharmacol. 2002 Jul;40(1):153-61.

Apamine was without effect on the CRC for all the PDEI used in this study. (1) PDE3, 4 and 5 are functionally present in human intralobar pulmonary arteries; (2) the vasoconstriction induced by U46619 is downregulated by 4-aminopyridine sensitive-K+ channels; (3) the relaxant effects of rolipram (PDE4I) are partly mediated through KATP, BKCa, and Kv potassium channels and those of siguazodan (PDE3I) by Kv potassium channels.
31(0,1,1,1) Details
15237094 Wu BN, Lin RJ, Lo YC, Shen KP, Wang CC, Lin YT, Chen IJ: KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14. Epub 2004 Jul 5.

Tracheal relaxation induced by KMUP-1 was attenuated by epithelium removal and by pretreatment with inhibitors of soluble guanylate cyclase (sGC) (1H-[1,2,4] oxadiazolo [4,3-a] quinoxalin-1-one (ODQ), 1 microm), nitric oxide synthase (Nomega-nitro-L-arginine methyl ester, 100 microm), K+ channels (tetraethylammonium, 10 mm), KATP channels (glibenclamide, 1 microm), voltage-dependent K+ channels (4-aminopyridine, 100 microm) and Ca2+-dependent K+ channels (charybdotoxin, 0.1 microm or apamin, 1 microm).
Both KMUP-1 (10 microm) and theophylline nonselectively and slightly inhibited the enzyme activity of PDE3, 4 and 5, suggesting that they are able to inhibit the metabolism of adenosine 3',5'-cyclic monophosphate (cyclic AMP) and guanosine 3',5'-cyclic monophosphate (cyclic GMP).
2(0,0,0,2) Details