To investigate whether the antivasoconstrictor effect of P1075, a potassium channel openers, could be partly due to modulation of neurotransmitter release from adrenergic nerve endings we analysed the presynaptic and postsynaptic effects of P1075 on the isolated human saphenous vein (HSV). The HSV rings were contracted by electrical field stimulation (EFS) or by exogenous noradrenaline (10 μM; NA). The repetitive transmural EFS was carried out at 20 Hz with square wave pulses of 0.3 ms duration and supramaximal voltage. The contraction of the HSV in response to transmural EFS recorded in our experiments are neurogenic in nature, as this effect was abolished by tetrodotoxin (1 μM). We have also found that phentolamine (1 μM) inhibited almost completly (90 ″ 2%) the HSV contractions to EFS suggesting that this response was mediated by NA release from perivascular sympathetic nerve endings activating postjuncional α adrenoceptors. P1075 (0.01-10 μM) induced a concentration-dependent inhib...ition of both neurogenic contractions, and contractions evoked by exogenous NA of the HSV with pEC 50 values of of 6.48 ″ 0.05 and 6.36″ 0.08. The difference between the pEC 50 values (r) was not statistically significant (P > 0.05). These results suggest that the antivasoconstrictor effect of P1075 on the HSV might be postsynaptic, and associated with opening of the smooth muscle potassium channels.
TY - JOUR
AU - Gojković-Bukarica, Ljiljana
AU - Kazić, T
AU - Beleslin Cokić, B
AU - Novaković, Aleksandra
AU - Perić, M
AU - Sajić, Zoran
AU - Bojić, M
AU - Đukanović, B
AU - Kanjuh, Vladimir
PY - 2000
UR - http://farfar.pharmacy.bg.ac.rs/handle/123456789/275
AB - To investigate whether the antivasoconstrictor effect of P1075, a potassium channel openers, could be partly due to modulation of neurotransmitter release from adrenergic nerve endings we analysed the presynaptic and postsynaptic effects of P1075 on the isolated human saphenous vein (HSV). The HSV rings were contracted by electrical field stimulation (EFS) or by exogenous noradrenaline (10 μM; NA). The repetitive transmural EFS was carried out at 20 Hz with square wave pulses of 0.3 ms duration and supramaximal voltage. The contraction of the HSV in response to transmural EFS recorded in our experiments are neurogenic in nature, as this effect was abolished by tetrodotoxin (1 μM). We have also found that phentolamine (1 μM) inhibited almost completly (90 ″ 2%) the HSV contractions to EFS suggesting that this response was mediated by NA release from perivascular sympathetic nerve endings activating postjuncional α adrenoceptors. P1075 (0.01-10 μM) induced a concentration-dependent inhibition of both neurogenic contractions, and contractions evoked by exogenous NA of the HSV with pEC 50 values of of 6.48 ″ 0.05 and 6.36″ 0.08. The difference between the pEC 50 values (r) was not statistically significant (P > 0.05). These results suggest that the antivasoconstrictor effect of P1075 on the HSV might be postsynaptic, and associated with opening of the smooth muscle potassium channels.
PB - BMJ Publishing Group
T2 - Heart
T1 - The antivasoconstrictor effect of P1075 on the isolated human saphenous vein
VL - 83
IS - SUPPL. 2
ER -
@article{
author = "Gojković-Bukarica, Ljiljana and Kazić, T and Beleslin Cokić, B and Novaković, Aleksandra and Perić, M and Sajić, Zoran and Bojić, M and Đukanović, B and Kanjuh, Vladimir",
year = "2000",
url = "http://farfar.pharmacy.bg.ac.rs/handle/123456789/275",
abstract = "To investigate whether the antivasoconstrictor effect of P1075, a potassium channel openers, could be partly due to modulation of neurotransmitter release from adrenergic nerve endings we analysed the presynaptic and postsynaptic effects of P1075 on the isolated human saphenous vein (HSV). The HSV rings were contracted by electrical field stimulation (EFS) or by exogenous noradrenaline (10 μM; NA). The repetitive transmural EFS was carried out at 20 Hz with square wave pulses of 0.3 ms duration and supramaximal voltage. The contraction of the HSV in response to transmural EFS recorded in our experiments are neurogenic in nature, as this effect was abolished by tetrodotoxin (1 μM). We have also found that phentolamine (1 μM) inhibited almost completly (90 ″ 2%) the HSV contractions to EFS suggesting that this response was mediated by NA release from perivascular sympathetic nerve endings activating postjuncional α adrenoceptors. P1075 (0.01-10 μM) induced a concentration-dependent inhibition of both neurogenic contractions, and contractions evoked by exogenous NA of the HSV with pEC 50 values of of 6.48 ″ 0.05 and 6.36″ 0.08. The difference between the pEC 50 values (r) was not statistically significant (P > 0.05). These results suggest that the antivasoconstrictor effect of P1075 on the HSV might be postsynaptic, and associated with opening of the smooth muscle potassium channels.",
publisher = "BMJ Publishing Group",
journal = "Heart",
title = "The antivasoconstrictor effect of P1075 on the isolated human saphenous vein",
volume = "83",
number = "SUPPL. 2"
}
Gojković-Bukarica, L., Kazić, T., Beleslin Cokić, B., Novaković, A., Perić, M., Sajić, Z., Bojić, M., Đukanović, B.,& Kanjuh, V. (2000). The antivasoconstrictor effect of P1075 on the isolated human saphenous vein.
Heart
BMJ Publishing Group., 83(SUPPL. 2).
Gojković-Bukarica L, Kazić T, Beleslin Cokić B, Novaković A, Perić M, Sajić Z, Bojić M, Đukanović B, Kanjuh V. The antivasoconstrictor effect of P1075 on the isolated human saphenous vein. Heart. 2000;83(SUPPL. 2)
Gojković-Bukarica Ljiljana, Kazić T, Beleslin Cokić B, Novaković Aleksandra, Perić M, Sajić Zoran, Bojić M, Đukanović B, Kanjuh Vladimir, "The antivasoconstrictor effect of P1075 on the isolated human saphenous vein" Heart, 83, no. SUPPL. 2 (2000)
