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Biomedical subjects

A I Fernandez

Publications and source records attributed to A I Fernandez.

5 recordsLinked to original sources

Effects of phorbol 12,13-dibutyrate and H-7 in extravascular smooth muscle contraction.

The effect of the activator, phorbol 12,13-dibutyrate (PDB), and the inhibitor, H-7, of protein kinase C (PKC) has been assayed in rat uterus. PDB increases the amplitude of spontaneous contractions of rat uterus and this effect does not occur in the presence of H-7 or nifedipine. PDB did not modify the KCl-induced tonic contraction but H-7 relaxed it, in a concentration-dependent way. PDB inhibited the contraction induced by oxytocin in rat uterus incubated in Ca-free solution and relaxed the tonic contraction induced by oxytocin in this medium. The relaxing effect of PDB on oxytocin-induced contraction was not modified by H-7. Thus H-7 relaxed, in a concentration-dependent way, the tonic contractions induced by oxytocin and vanadate in the rat uterus incubated in Ca-free medium. Our results suggest a dual effect of PDB related to calcium, and a direct and PKC-independent inhibitory effect of H-7.

1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine

Mediators involved in the rat uterus contraction in calcium-free solution.

1. The effect of (Na+ + K+)-ATPase inhibitor ouabain (10(-5)-3 x 10(-4) M), and the (Ca2+ + Mg2+)-ATPase inhibitors vanadate (6 x 10(-6)-6 x 10(-4) M), oxytocin (2 x 10(-9)-4 x 10(-8) M, and prostaglandin F2 alpha (PGF2 alpha, 10(-7)-6 x 10(-6) M) were assayed on rat uterus incubated in Ca-free medium. 2. Vanadate, oxytocin and PGF2 alpha, but not ouabain, induced contractions in a dose-dependent way (ED50: 7.5 +/- 0.03 x 10(-5) M; 6.5 +/- 0.064 x 10(-9) M and 3.8 +/- 0.085 x 10(-7) M). 3. Vanadate (3 x 10(-4) M) and oxytocin (OT, 10 mU/ml = 2 x 10(-8) M)-induced tonic contraction were not modified by nifedipine (10(-10)-10(-6) M), monensin (10(-5)-3 x 10(-4) M) or amiloride (10(-5)-10(-3) M). 4. The intracellular calcium release inhibitors TMB-8 (10(-6)-10(-4) M) and dantrolene (3 x 10(-6)-10(-4) M), and the prostaglandin release inhibitor indomethacin (3 x 10(-8)-6 x 10(-5) M) relaxed the vanadate and OT-induced tonic contractions. 5. The calmodulin inhibitors trifluoperazine (3 x 10(-5)-3 x 10(-4) M), bepridil (10(-8)-3 x 10(-4) M), calmidazolium (10(-7)-10(-4) M) and W-7 (10(-7)-10(-5) M) also relaxed the vanadate and OT-induced tonic contractions. 6. Our results suggest that oxytocin and vanadate-induced contractions on rat uterus in Ca-free medium could be produced by release of prostaglandins and intracellular calcium, and mediated by calmodulin.

Animals

Differential effect of calcium and Bay K 8644 on the inhibitory action of estrogens in the rat uterus.

1. The effects of the estrogens estradiol (E2, 10(-7) to 3 x 10(-5) M) and diethylstilbestrol (DES, 10(-7) to 3 x 10(-6) M) on tonic contractions of the rat uterus induced by KCl and CaCl2 have been studied. 2. E2 and DES relaxed, in a dose-dependent way, the tonic contraction induced by KCl (60 mM) (IC50: 5.16 +/- 1.49 x 10(-6) and 4.51 +/- 0.03 x 10(-7) M); the tonic contraction induced by CaCl2 (3 mM) in the rat uterus incubated in depolarizing Krebs (127 mM of K+) have also been relaxed (IC50: 8.6 +/- 0.03 x 10(-7) and 2.56 +/- 0.07 x 10 M) by both drugs. 3. The CaCl2 (0.1 to 10 mM) counteracted the relaxing effect of E2 and DES, respectively, up to 28.13 +/- 10.2% and 34.71 +/- 11.5%, on KCl-induced contractions, and up to 126.36 +/- 19.35% and 95.8 +/- 16.3% on CaCl2-induced contractions. 4. Bay K 8644 (10(-10) to 10(-6) M) reversed the relaxing effect of E2 and DES, respectively, up to 42.49 +/- 2.28% and 43.31 +/- 3.59% on KCl-induced contractions, and up to 21.73 +/- 4.16% and 75.97 +/- 9.63% on CaCl2-induced contractions. 5. Propranolol (10(-6) M) did not modify the relaxing effect of E2 or DES on CaCl2-induced contractions.

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy