4. reseptor kanal ion concise.pptx
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Transcript of 4. reseptor kanal ion concise.pptx
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Target aksi Obat
1. Proteina. Kanal ionb. Transporter/Carriers/pembawac. Enzimd. Reseptor
i. Reseptor Kanal ion/Ligand-gated ion channel receptor
ii. G protein coupled receptoriii. Tyrosine kinase-linked receptoriv. Reseptor intraseluler/nuclear receptor
2. DNA
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This ppt modified from Ikawati Z., 2008
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Many basic principles of chemical transmission were discovered at the neuromuscular junction (nerve-muscle synapse,endplate); acetylcholine is the transmitter.
Figure 11-1
From Lecture 4
10
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0.3 µm
Fine structure of the NMJ
Figure 11-1
From Lecture 4
11
ACh receptors
Incl. acetylcholinesterase
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Arrangement of subunits in the muscle nicotinic ACh receptor
Karlin Nature Rev. Neurosci. 3: 102 (2002)Keramidas et al., Prog. Biophys. Mol. Biol.86: 161 (2004)
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Apa hubungannya dengan Na+?
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Tipe Reseptor GABA
GABA a sudah banyak di eksplorasi, terkait kanal ion Cl-, dapat diblok dengan bicuculin, dapat dimodulasi oleh benzodiazepin, barbiturat, steroid
GABA b metabotropik (via GPCR) GABA c sama2 terkait kanal Cl-,
namun tidak dapat diblok dengan bicuculin, tidak dapat dimodulasi oleh benzodiazepin, barbiturat, steroid
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Receptor site Penempelan ligan GABA pada reseptor Kanal
ion Cl- terbuka hiperpolarisasi menghambat penghantaran potensial aksi
Mekanisme sebagai neurotransmitter inhibitor: depresi CNS (sedatif, hipnotik, antikonvulsan)
Antagonis: konvulsi Misal: pitrazepin, securinin, gabazin Antagonis tapi di binding site yang berbeda:
pikrotoksin
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Benzodiazepine site
Obat ini meningkatkan afinitas reseptor terhadap GABA pada tempat ikatannya sehingga meningkatkan frekuensi pembukaan kanal ion Cl-.
Obat inverse agonist: b-karbolin. Efeknya berkebalikan
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Barbiturat site
Barbiturat memperpanjang durasi pembukaan kanal sehingga memaksimalkan kesempatan bagi Cl- mengalir
Kerja etanol, anastetik volatil serupa di atas
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Steroid site
Neurosteroid/ neuroaktif Neurosteroid: suatu senyawa steroid
yang disintesis oleh sel glia di otak Steroid neuroaktif: suatu senyawa
steroid, baik yang disintesis di otak maupun perifer, yang beraksi pada eksitabilitas saraf.
Istlah bisa saling dipertukarkan
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