Selamat Datang di Kuliah Farmakologi Molekuler
Obat dapat didefinisikan
suatu agen kimia yang secara unik berinteraksi dengan molekul target spesifik dalam tubuh dan menghasilkan efek biologis
Mekanisme Aksi Obat
• Aksi non-spesifik
• Aksi spesifik:
• - enzim
• - kanal ion
• - molekul pembawa/transporter
• - reseptor
Target Aksi Obat
Kebanyakan target aksi terletak pada membran sel Sebagian besar reseptor adalah reseptor membran ada di permukaan Beberapa target aksi obat terdapat pada daerah intraseluler : reseptor intraseluler, enzim, nukleus
Review Biologi Sel
Target aksi Obat
1. Protein
a. Kanal ion
b. Transporter/Carriers/pembawa
c. Enzim
d. Reseptor
i. Reseptor Kanal ion/Ligand-gated ion channel receptor
ii. G protein coupled receptor
iii. Tyrosine kinase-linked receptor
iv. Reseptor intraseluler/nuclear receptor
2. DNA
Ion Channal Used as Drug Target
• Ion Channal: Calcium Ion Channal, Potassium
Ion Channal, Sodium Ion Channal, Chloride Ion
Channal, etc.
• Drugs effecting on Ion Channal: Calcium Channal
Blocker, Potassium Channal Blocker, Sodium
Channal Blocker, etc.
7
Enzyme Used as Drug Target
• Enzyme: Angiotensin Converting Enzyme
(ACE), Cycloxygenase（COX2），β-
Lactamase, Acetylcholine Esterase etc.
• Drugs effecting on enzyme: Enzyme Inhibitor
8
Receptor Used as Drug Target
• Receptors: ligand gate-ion channel, GPCR, RTK, nuclear
receptor
• Example: acetylcholine receptor; adrenergic receptor;
angiotensin receptor; dopamine receptor; serotonin
receptor; opioid receptor etc.
• Drugs effecting on receptors：Agonist；Antagonist
Drug
Receptor
9
• Agonist is an endogenous substance or a drug
that can interact with a receptor and initiate a
physiological or a pharmacological response
(contraction, relaxation, secretion, enzyme
activation, etc.).
• Antagonist is a drug or a compound that
opposes the receptor-associated responses
normally induced by another bioactive agent.
• Partial agonist is an agonist which is unable to
induce maximal activation of a receptor
population, regardless of the amount of drug
applied.
10
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Tipe Reseptor
GPCRs
Growth Factor Receptors
Ligand-gated
Ion Channel receptor
Nuclear receptors
Transport
Receptors
1
2
3
4
Senyawa Endogenous beraksi pada reseptornya
Neurotransmitter
Neuropeptida
Hormon
Ion
• Obat, sebagaimana hormon, neurotransmitter dan toksin memungkin terjadinya transfer informasi ke sel denganbeinteraksi dengan molekul spesifik di sebut “reseptor”.
Ligand-gated Ion-Channel Receptors
G Protein–linked Receptors
Tyrosine kinase-linked receptor (Enzyme-like Receptors)
Nuclear Receptors
