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Nicotinic Acetylcholine Receptor (nAChR) Competitive Modulators/Agonists

Bahuddin Zakariya University, Multan
Bahuddin Zakariya University, Multan
Bahuddin Zakariya University, MultanStudent at University of Sargodha

This Presentation is all about Nicotinic Acetylcholine Receptor (nAChR) Competitive Modulators (Agonists). All points are explained by diagrammatically. If you need any help about this topic, then mail me on mzeeshan_93@yahoo.com

Nicotinic Acetylcholine Receptor (nAChR) Competitive Modulators/Agonists

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Nicotinic Acetylcholine Receptor (nAChR)
Competitive Modulators/Agonists
Department of Agriculture Entomology Bahauddin Zakariya University, Multan
By: Muhammad Zeeshan Nazar
Email ID: mzeeshan_93@yahoo.com
• Neurotransmitters are Chemical Messengers that communicate
information throughout the body by neural system.
• They are found at the terminal region of axon in the synaptic vesicles.
• Acetylcholine neurotransmitters are involved in
 Contraction of skeletal muscles.
 Activate glandular functions in the endocrine system.
 Sensation of pain.
Acetylcholine Neurotransmitter
• Receptor proteins respond to the neurotransmitter, acetylcholine.
• Nicotinic Acetylcholine Receptors also respond to drugs, including the
Nicotinic Receptor Agonist.
• They are found in the CNS and PNS, muscle and
many other tissues of many organisms.
• In insects, limited to the central nervous system.
• Transmit outgoing signals from the presynaptic to
the postsynaptic cells.
Nicotinic Acetylcholine Receptors (nAChRs)
Agonist
nAChR
Nicotinic Acetylcholine Receptor (nAChR) Competitive Modulators/Agonists
Receptor sites
Synaptic Vesicles
• Neuro-active, systemic insecticides.
• Mimics the action of acetylcholine at nAChRs.
• Chemically bind to acetylcholine receptors site.
 Block acetylcholine access to receptor sites.
• Continuous sending unwarranted neural transmissions.
• Receptors and cells involved in neural transmission become exhausted
and fail to function.
• Results in paralysis and death of insects.
Nicotinic Acetylcholine Receptors Competitive Modulators/Agonist
Mode of Action
Ad

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Nicotinic Acetylcholine Receptor (nAChR) Competitive Modulators/Agonists

  • 1. Nicotinic Acetylcholine Receptor (nAChR) Competitive Modulators/Agonists Department of Agriculture Entomology Bahauddin Zakariya University, Multan By: Muhammad Zeeshan Nazar Email ID: mzeeshan_93@yahoo.com
  • 2. • Neurotransmitters are Chemical Messengers that communicate information throughout the body by neural system. • They are found at the terminal region of axon in the synaptic vesicles. • Acetylcholine neurotransmitters are involved in  Contraction of skeletal muscles.  Activate glandular functions in the endocrine system.  Sensation of pain. Acetylcholine Neurotransmitter
  • 3. • Receptor proteins respond to the neurotransmitter, acetylcholine. • Nicotinic Acetylcholine Receptors also respond to drugs, including the Nicotinic Receptor Agonist. • They are found in the CNS and PNS, muscle and many other tissues of many organisms. • In insects, limited to the central nervous system. • Transmit outgoing signals from the presynaptic to the postsynaptic cells. Nicotinic Acetylcholine Receptors (nAChRs) Agonist nAChR
  • 6. • Neuro-active, systemic insecticides. • Mimics the action of acetylcholine at nAChRs. • Chemically bind to acetylcholine receptors site.  Block acetylcholine access to receptor sites. • Continuous sending unwarranted neural transmissions. • Receptors and cells involved in neural transmission become exhausted and fail to function. • Results in paralysis and death of insects. Nicotinic Acetylcholine Receptors Competitive Modulators/Agonist Mode of Action
  • 7. Vesicles of acetylcholine Insecticide Nicotine receptors blocked Constant neuromuscular stimulation
  • 8. 1. Neonicotinoids • Acetamiprid • Imidacloprid • Nitenpyram • Thiacloprid • Thiamethoxam • Clothianidin 2. Sulfoximines • Sulfoxaflor Examples
  • 9. References Thomas, C. S., et al. 2013. Sulfoxaflor and the sulfoximine insecticides: Chemistry, mode of action and basis for efficacy on resistant insects. Pesticide Biochemistry and Physiology Lopez, O. and Fernandez, J.G. Green Trends in Insect Control. Royal Society of Chemistry. Cambridge, UK. pp. 132–162. Tomizawa, M., Casida, J.E. 2011. Unique neonicotinoid binding conformations conferring selective receptor interactions. Agric. Food. Chem. 59: 2825–2828. Simon, D.N. 2015. Systemic insecticides (neonicotinoids and fipronil): trends, uses, mode of action and metabolites. Environ Sci Pollut Res. Vol. 22:5–34 Wagner, S. 2016. Environmental Fate of Imidacloprid. Environmental Monitoring Branch Department of Pesticide Regulation Fishel, F.M. 2005. Evaluation of pesticides for carcinogenic potential. PI-37. Gainesville: University of Florida Institute of Food and Agricultural Sciences.