Brief application of AF2 produces long lasting potentiation of nAChR responses in Ascaris suum
Само за регистроване кориснике
2005
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Resistance of parasitic nematodes to the cholinergic anthelmintic levamisole is associated with a reduction in the proportion of time
that acetylcholine receptor ion-channels are in the open state decreasing the response of nematode parasites to the drug. Here we examine
electrophysiological and contractile responses to acetylcholine and the cholinergic agonist, levamisole, in Ascaris suum muscle looking
for a pharmacological approach that may be developed to increase the response to cholinergic agonists. We found that short application
of the FMRFamide, AF2, produced modulation (long lasting potentiation) of the peak membrane potential response to acetylcholine but
not to levamisole. Since levamisole preferentially activates L-type acetylcholine receptors, we also tested the effect of nicotine (selective
activator of N-type acetylcholine receptors) and bephenium (selective activator of B-type acetylcholine receptors) and found again no effect
of AF2 on peak membrane potential r...esponses. We then tested atropine on the AF2 potentiation of acetylcholine and found it to inhibit
the peak potentiation suggesting that AF2 receptors interact with muscarinic receptors to produce the potentiation of acetylcholine. We saw
similar atropine sensitive potentiation of acetylcholine responses in our muscle contraction experiments. The potentiation of the acetylcholine
responses shows that nematode acetylcholine receptors are capable of a level of plasticity. A model involving calcium release from the
sarcoplasmic reticulum, CaM Kinase, calcineurin, muscarinic receptors and AF2 receptors is proposed to explain our observations. These
observations are important because they point to a pharmacological approach that may be developed to counter resistance to cholinergic
anthelmintics.
Кључне речи:
AF2; Acetylcholine; Levamisole; Ascaris; Electrophysiology; PotentiationИзвор:
Molecular & Biochemical Parasitology, 2005, 139, 51-64Издавач:
- Elsevier B.V.
Финансирање / пројекти:
- NIH R.J.M.: RO1 A147194-02
Институција/група
Fakultet veterinarske medicineTY - JOUR AU - Trailović, Saša AU - Cheryl, L. Clark AU - Alan, P. Robertson AU - Richard, J. Martin PY - 2005 UR - https://vet-erinar.vet.bg.ac.rs/handle/123456789/2626 AB - Resistance of parasitic nematodes to the cholinergic anthelmintic levamisole is associated with a reduction in the proportion of time that acetylcholine receptor ion-channels are in the open state decreasing the response of nematode parasites to the drug. Here we examine electrophysiological and contractile responses to acetylcholine and the cholinergic agonist, levamisole, in Ascaris suum muscle looking for a pharmacological approach that may be developed to increase the response to cholinergic agonists. We found that short application of the FMRFamide, AF2, produced modulation (long lasting potentiation) of the peak membrane potential response to acetylcholine but not to levamisole. Since levamisole preferentially activates L-type acetylcholine receptors, we also tested the effect of nicotine (selective activator of N-type acetylcholine receptors) and bephenium (selective activator of B-type acetylcholine receptors) and found again no effect of AF2 on peak membrane potential responses. We then tested atropine on the AF2 potentiation of acetylcholine and found it to inhibit the peak potentiation suggesting that AF2 receptors interact with muscarinic receptors to produce the potentiation of acetylcholine. We saw similar atropine sensitive potentiation of acetylcholine responses in our muscle contraction experiments. The potentiation of the acetylcholine responses shows that nematode acetylcholine receptors are capable of a level of plasticity. A model involving calcium release from the sarcoplasmic reticulum, CaM Kinase, calcineurin, muscarinic receptors and AF2 receptors is proposed to explain our observations. These observations are important because they point to a pharmacological approach that may be developed to counter resistance to cholinergic anthelmintics. PB - Elsevier B.V. T2 - Molecular & Biochemical Parasitology T1 - Brief application of AF2 produces long lasting potentiation of nAChR responses in Ascaris suum VL - 139 SP - 51 EP - 64 DO - 10.1016/j.molbiopara.2004.10.001 ER -
@article{ author = "Trailović, Saša and Cheryl, L. Clark and Alan, P. Robertson and Richard, J. Martin", year = "2005", abstract = "Resistance of parasitic nematodes to the cholinergic anthelmintic levamisole is associated with a reduction in the proportion of time that acetylcholine receptor ion-channels are in the open state decreasing the response of nematode parasites to the drug. Here we examine electrophysiological and contractile responses to acetylcholine and the cholinergic agonist, levamisole, in Ascaris suum muscle looking for a pharmacological approach that may be developed to increase the response to cholinergic agonists. We found that short application of the FMRFamide, AF2, produced modulation (long lasting potentiation) of the peak membrane potential response to acetylcholine but not to levamisole. Since levamisole preferentially activates L-type acetylcholine receptors, we also tested the effect of nicotine (selective activator of N-type acetylcholine receptors) and bephenium (selective activator of B-type acetylcholine receptors) and found again no effect of AF2 on peak membrane potential responses. We then tested atropine on the AF2 potentiation of acetylcholine and found it to inhibit the peak potentiation suggesting that AF2 receptors interact with muscarinic receptors to produce the potentiation of acetylcholine. We saw similar atropine sensitive potentiation of acetylcholine responses in our muscle contraction experiments. The potentiation of the acetylcholine responses shows that nematode acetylcholine receptors are capable of a level of plasticity. A model involving calcium release from the sarcoplasmic reticulum, CaM Kinase, calcineurin, muscarinic receptors and AF2 receptors is proposed to explain our observations. These observations are important because they point to a pharmacological approach that may be developed to counter resistance to cholinergic anthelmintics.", publisher = "Elsevier B.V.", journal = "Molecular & Biochemical Parasitology", title = "Brief application of AF2 produces long lasting potentiation of nAChR responses in Ascaris suum", volume = "139", pages = "51-64", doi = "10.1016/j.molbiopara.2004.10.001" }
Trailović, S., Cheryl, L. C., Alan, P. R.,& Richard, J. M.. (2005). Brief application of AF2 produces long lasting potentiation of nAChR responses in Ascaris suum. in Molecular & Biochemical Parasitology Elsevier B.V.., 139, 51-64. https://doi.org/10.1016/j.molbiopara.2004.10.001
Trailović S, Cheryl LC, Alan PR, Richard JM. Brief application of AF2 produces long lasting potentiation of nAChR responses in Ascaris suum. in Molecular & Biochemical Parasitology. 2005;139:51-64. doi:10.1016/j.molbiopara.2004.10.001 .
Trailović, Saša, Cheryl, L. Clark, Alan, P. Robertson, Richard, J. Martin, "Brief application of AF2 produces long lasting potentiation of nAChR responses in Ascaris suum" in Molecular & Biochemical Parasitology, 139 (2005):51-64, https://doi.org/10.1016/j.molbiopara.2004.10.001 . .