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