Receptor imaging in the thorax with PET.
This review focuses on positron emission tomography (PET)-imaging of receptors in the sympathetic and the parasympathetic systems of heart and lung and highlights the human applications of PET. For the alpha-adrenoceptor, only [11C]GB67 (N2-[6-[(4-amino-6,7-dimethoxy-2-quinazolinyl)(methyl)amino]hexyl]-N2-[11C]methyl-2-furamide hydrochloride) has been developed. Its potential for application in patients needs to be assessed. For both the beta-adrenergic and the muscarinic systems, potent PET radioligands have been prepared and evaluated in patients. It has been possible to measure receptor densities quantitatively in human heart [[11C]MQNB: [11C]methylquinuclidinyl benzilate, [11C]CGP12177: S-(3'-t-butylamino-2'-hydroxypropoxy)-benzimidazol-2-[11C]one and [11C]CGP12388: (S)-4-(3-(2'-[11C]isopropylamino)-2-hydroxypropoxy)-2H-benzimidazol-2-one] and qualitatively in lung [[11C]VC002: N-[11C]-methyl-piperidin-4-yl-2-cyclohexyl-2-hydroxy-2-phenylacetate and [11C]CGP12177]. Besides these subtype nonselective radioligands, the development of compounds that are selective for one subtype are ongoing and have not found successful application in humans yet.
Elsinga
Philip H
PH
Groningen University Hospital, PET-center, P.O. Box 30001, 9700 RB Groningen, The Netherlands. p.h.elsinga@pet.azg.nl
van Waarde
Aren
A
Vaalburg
Willem
W
D000316:Adrenergic alpha-Agonists / Q000378:metabolism; D000317:Adrenergic alpha-Antagonists / Q000378:metabolism; D000318:Adrenergic beta-Agonists / Q000378:metabolism; D000319:Adrenergic beta-Antagonists / Q000378:metabolism; D000818:Animals; D001562:Benzimidazoles / Q000378:metabolism; D002227:Carbazoles / Q000378:metabolism; D002250:Carbon Radioisotopes; D004983:Ethanolamines / Q000378:metabolism; D000068759:Formoterol Fumarate; D006801:Humans; D049268:Positron-Emission Tomography / Q000379:methods*; D011412:Propanolamines / Q000378:metabolism; D011869:Radioligand Assay; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism*; D011943:Receptors, Adrenergic, beta / Q000378:metabolism*; D013909:Thorax / Q000000981:diagnostic imaging* / Q000378:metabolism
D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D001562:Benzimidazoles; D002227:Carbazoles; D002250:Carbon Radioisotopes; D004983:Ethanolamines; D011412:Propanolamines; D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; C109239:CGP 12388; C089702:fluorocarazolol; C033394:CGP 12177; D000068759:Formoterol Fumarate