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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.
b.
c.
d.

2. DNA

Kanal ion
Transporter/Carriers/pembawa
Enzim
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

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.

Enzyme Used as Drug Target

Enzyme: Angiotensin Converting Enzyme
(ACE),
CycloxygenaseCOX2Lactamase, Acetylcholine Esterase etc.
Drugs effecting on enzyme: Enzyme Inhibitor

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 receptorsAgonistAntagonist
Receptor

Drug

 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

11

Tipe Reseptor

Growth Factor Receptors

Transport
Receptors

2
GPCRs

Nuclear receptors

4
1

Ligand-gated
Ion Channel receptor

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 Proteinlinked Receptors

Tyrosine kinase-linked receptor

(Enzyme-like Receptors)

Nuclear Receptors