DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table 3–1
Physiological Receptors
STRUCTURAL FUNCTIONAL PHYSIOLOGICAL EFFECTORS AND
FAMILY FAMILY LIGANDS TRANSDUCERS EXAMPLE DRUGS
β Adrenergic NE, Epi, DA G s
; AC Dobutamine,
receptors
propranolol
GPCR
Muscarinic ACh G i
and G q
; AC, Atropine
cholinergic receptors
ion channels, PLC
Eicosanoid receptors Prostaglandins, G s
, G i
and G q
proteins Misoprostol,
leukotrienes,
montelukast
thromboxanes
Thrombin receptors Receptor peptide G 12/13
, GEFs (in development)
(PAR)
Ion channels Ligand-gated ACh (M 2
), Na + , Ca 2+ , K + , Cl − Nicotine, gabapentin
GABA, 5-HT
Voltage-gated None (activated Na + , Ca 2+ , K + , Lidocaine, verapamil
by membrane
other ions
depolarization)
Transmembrane Receptor tyrosine Insulin, PDGF, EGF, SH2 domain and PTB- Herceptin, imatinib
enzymes kinases VEGF, growth factors containing proteins
Membrane-bound GC Natriuretic peptides Cyclic GMP Neseritide
Tyrosine phosphatases
Transmembrane, Cytokine receptors Interleukins and Jak/STAT, soluble
non-enzymes other cytokines tyrosine kinases
Toll-like receptors LPS, bacterial products MyD88, IARKs, NF-κB
Nuclear receptors Steroid receptors Estrogen, testosterone Co-activators Estrogens,
androgens, cortisol
Thyroid hormone Thyroid hormone Thyroid hormone
receptors
PPARγ PPARγ Thiazolidinediones
Intracellular Soluble GC NO, Ca 2+ Cyclic GMP Nitrovasodilators
enzymes
AC, adenylyl cyclase; GC, guanylyl cyclase; PAR, protease-activated receptor; PLC, phospholipase C; PPAR, peroxisome proliferator-activated
receptor.
its action on muscarinic receptors. NE released by the
sympathetic nervous system interacts with α and β
adrenergic receptors to regulate cardiac function and the
tone of vascular smooth muscle (Chapters 8-12).
Because of their number and physiological importance,
GPCRs are the targets for many drugs; perhaps
half of all non-antibiotic prescription drugs act at these
receptors.
Receptor Subtypes. There are multiple receptor subtypes
within families of receptors. Ligand-binding studies
with multiple chemical entities initially identified
receptor subtypes; molecular cloning has greatly accelerated
the discovery and definition of additional receptor
subtypes; their expression as recombinant proteins
has facilitated the discovery of subtype-selective drugs.
Distinct but related receptors may display distinctive