Drugs That Interact with Receptors and Ion Channels
Pp. 390-415 (26)
Robert E. Smith
There are many important drugs that bind receptors. Morphine, codeine and
heroin and fentanyl bind to opioid receptors. Barbituates, zolpidem and diazepam bind
to GABAA receptors. Varenicline binds to nicotinic acetylcholine receptors; Tiotropium
bromide binds to the M3 muscarinic acetylcholine receptor. Tamsulin binds α1aadrenergic
receptors in the prostate; bronchodilators bind to β2-adrenergic receptors.
Ramelteon binds to the melatonin receptor and lets the patient sleep. Memantine binds
to the NMDA subset of glutamate receptors. Montelukast sodium is a synthetic
antagonist of a cysteinyl leukotriene receptor. Loratadine blocks the binding of
histamine to its receptor. Prostaglandin analogs, such as latanoprost decrease intraocular
pressure by binding to prostaglandin receptors. Ranitidine binds to the histamine H2
receptor. Glipizide binds to K+ ion channels in the β cells of the pancreas. Pioglitazone
is an agonist of the peroxisome proliferator-activated receptor-γ, or PPARγ. Atenolol
binds competitively to the β-adrenergic receptor and blocks the binding of the natural
ligands, adrenaline and noradrenaline. Calcium ion channel blockers like Amlodipine
decrease contractions of the heart and dilate the arteries, lowering blood pressure.
Clopidogrel bisulfate prevents the formation of blood clots by inhibiting the binding of
ADP to its platelet receptor. Estrogens and progestins bind to estrogen receptors and
progesterone binds to its receptor. Oxytocin binds to G-protein coupled receptors
(GPCRs). Calcitriol binds to the Vitmin D receptor. Raloxifene is a selective estrogen
receptor modulator. FY720 binds to the sphingosine-1-phosphate receptor. Vaccine
adjuvants bind to toll-like receptors. UK-427857 (Maraviroc®) binds to the CCR5
receptor, preventing the binding of HIV.
GABAA, glutamate, prostaglandin, -adrenergic, platelet, Vitmin D,
estrogen, progesterone, M3 muscarinic acetylcholine, receptor, GPCR.
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