Paraherquamide and 2-Deoxy-paraherquamide Distinguish Cholinergic Receptor Subtypes in Ascaris Muscle
Само за регистроване кориснике
2002
Аутори
Robertson, P. AlanClark, Cheril L.
Burns, Teresa A.
Thompson, David P.
Geary, Timothy G.
Trailović, Saša
Martin, Richard J.
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Paraherquamide is a novel natural anthelmintic product with a
mode of action that is incompletely characterized. Nicotine and
cholinergic-anthelmintic agonists of different chemical classes
were used to produce contraction in Ascaris muscle strips.
Paraherquamide and a semisynthetic derivative, 2-deoxy-paraherquamide, antagonized these responses. Analysis of the actions of the antagonists was made using the simple competitive
model and nonlinear regression to estimate the pKB values of
the antagonists. The analysis was tested using Clark plots. The
pKB values for paraherquamide were: nicotine, 5.86 0.14;
levamisole, 6.61 0.19; pyrantel, 6.50 0.11; and bephenium,
6.75 0.15. The pKB of nicotine was significantly different from
the pKB values for levamisole, pyrantel, and bephenium, showing that paraherquamide can distinguish a subtype of cholinergic receptors sensitive to nicotine and a subtype of cholinergic receptors sensitive to levamisole, pyrantel, and
bephenium. ...The pKB values for 2-deoxy-paraherquamide were:
levamisole, 5.31 0.13; pyrantel, 5.63 0.10; and bephenium,
6.07 0.13. The Clark plots of the antagonism illustrated the
degree of fit to the competitive model for 2-deoxy-paraherquamide. 2-Deoxy-paraherquamide selectively antagonized the effects of bephenium; the pKB values of levamisole and pyrantel
were significantly different from the pKB of bephenium. Paraherquamide and 2-deoxy-paraherquamide are selective competitive cholinergic antagonists that distinguish subtypes of
cholinergic receptor in Ascaris muscle corresponding to nicotine-, levamisole-, and bephenium-sensitive receptors.
Кључне речи:
Paraherquamide / nicotine / levamisole / bephenium / Ascaris suumИзвор:
Journal of Pharmacology and Experimental Therapeutics, 2002, 302, 3, 853-860Издавач:
- American Society for Pharmacology and Experimental Therapeutics (ASPET)
Финансирање / пројекти:
- RO1 A147194-02 awarded R.J.M.
Институција/група
Fakultet veterinarske medicineTY - JOUR AU - Robertson, P. Alan AU - Clark, Cheril L. AU - Burns, Teresa A. AU - Thompson, David P. AU - Geary, Timothy G. AU - Trailović, Saša AU - Martin, Richard J. PY - 2002 UR - https://vet-erinar.vet.bg.ac.rs/handle/123456789/2623 AB - Paraherquamide is a novel natural anthelmintic product with a mode of action that is incompletely characterized. Nicotine and cholinergic-anthelmintic agonists of different chemical classes were used to produce contraction in Ascaris muscle strips. Paraherquamide and a semisynthetic derivative, 2-deoxy-paraherquamide, antagonized these responses. Analysis of the actions of the antagonists was made using the simple competitive model and nonlinear regression to estimate the pKB values of the antagonists. The analysis was tested using Clark plots. The pKB values for paraherquamide were: nicotine, 5.86 0.14; levamisole, 6.61 0.19; pyrantel, 6.50 0.11; and bephenium, 6.75 0.15. The pKB of nicotine was significantly different from the pKB values for levamisole, pyrantel, and bephenium, showing that paraherquamide can distinguish a subtype of cholinergic receptors sensitive to nicotine and a subtype of cholinergic receptors sensitive to levamisole, pyrantel, and bephenium. The pKB values for 2-deoxy-paraherquamide were: levamisole, 5.31 0.13; pyrantel, 5.63 0.10; and bephenium, 6.07 0.13. The Clark plots of the antagonism illustrated the degree of fit to the competitive model for 2-deoxy-paraherquamide. 2-Deoxy-paraherquamide selectively antagonized the effects of bephenium; the pKB values of levamisole and pyrantel were significantly different from the pKB of bephenium. Paraherquamide and 2-deoxy-paraherquamide are selective competitive cholinergic antagonists that distinguish subtypes of cholinergic receptor in Ascaris muscle corresponding to nicotine-, levamisole-, and bephenium-sensitive receptors. PB - American Society for Pharmacology and Experimental Therapeutics (ASPET) T2 - Journal of Pharmacology and Experimental Therapeutics T1 - Paraherquamide and 2-Deoxy-paraherquamide Distinguish Cholinergic Receptor Subtypes in Ascaris Muscle VL - 302 IS - 3 SP - 853 EP - 860 DO - DOI: 10.1124/jpet.102.034272. ER -
@article{ author = "Robertson, P. Alan and Clark, Cheril L. and Burns, Teresa A. and Thompson, David P. and Geary, Timothy G. and Trailović, Saša and Martin, Richard J.", year = "2002", abstract = "Paraherquamide is a novel natural anthelmintic product with a mode of action that is incompletely characterized. Nicotine and cholinergic-anthelmintic agonists of different chemical classes were used to produce contraction in Ascaris muscle strips. Paraherquamide and a semisynthetic derivative, 2-deoxy-paraherquamide, antagonized these responses. Analysis of the actions of the antagonists was made using the simple competitive model and nonlinear regression to estimate the pKB values of the antagonists. The analysis was tested using Clark plots. The pKB values for paraherquamide were: nicotine, 5.86 0.14; levamisole, 6.61 0.19; pyrantel, 6.50 0.11; and bephenium, 6.75 0.15. The pKB of nicotine was significantly different from the pKB values for levamisole, pyrantel, and bephenium, showing that paraherquamide can distinguish a subtype of cholinergic receptors sensitive to nicotine and a subtype of cholinergic receptors sensitive to levamisole, pyrantel, and bephenium. The pKB values for 2-deoxy-paraherquamide were: levamisole, 5.31 0.13; pyrantel, 5.63 0.10; and bephenium, 6.07 0.13. The Clark plots of the antagonism illustrated the degree of fit to the competitive model for 2-deoxy-paraherquamide. 2-Deoxy-paraherquamide selectively antagonized the effects of bephenium; the pKB values of levamisole and pyrantel were significantly different from the pKB of bephenium. Paraherquamide and 2-deoxy-paraherquamide are selective competitive cholinergic antagonists that distinguish subtypes of cholinergic receptor in Ascaris muscle corresponding to nicotine-, levamisole-, and bephenium-sensitive receptors.", publisher = "American Society for Pharmacology and Experimental Therapeutics (ASPET)", journal = "Journal of Pharmacology and Experimental Therapeutics", title = "Paraherquamide and 2-Deoxy-paraherquamide Distinguish Cholinergic Receptor Subtypes in Ascaris Muscle", volume = "302", number = "3", pages = "853-860", doi = "DOI: 10.1124/jpet.102.034272." }
Robertson, P. A., Clark, C. L., Burns, T. A., Thompson, D. P., Geary, T. G., Trailović, S.,& Martin, R. J.. (2002). Paraherquamide and 2-Deoxy-paraherquamide Distinguish Cholinergic Receptor Subtypes in Ascaris Muscle. in Journal of Pharmacology and Experimental Therapeutics American Society for Pharmacology and Experimental Therapeutics (ASPET)., 302(3), 853-860. https://doi.org/DOI: 10.1124/jpet.102.034272.
Robertson PA, Clark CL, Burns TA, Thompson DP, Geary TG, Trailović S, Martin RJ. Paraherquamide and 2-Deoxy-paraherquamide Distinguish Cholinergic Receptor Subtypes in Ascaris Muscle. in Journal of Pharmacology and Experimental Therapeutics. 2002;302(3):853-860. doi:DOI: 10.1124/jpet.102.034272. .
Robertson, P. Alan, Clark, Cheril L., Burns, Teresa A., Thompson, David P., Geary, Timothy G., Trailović, Saša, Martin, Richard J., "Paraherquamide and 2-Deoxy-paraherquamide Distinguish Cholinergic Receptor Subtypes in Ascaris Muscle" in Journal of Pharmacology and Experimental Therapeutics, 302, no. 3 (2002):853-860, https://doi.org/DOI: 10.1124/jpet.102.034272. . .