Biomaterial Database

Synthesis and in vivo distribution in the rat of several fluorine-18 labeled N-fluoroalkylaporphines. 1993

S Zijlstra, and G M Visser, and J Korf, and W Vaalburg

PET Center, GCCS, Groningen, The Netherlands.

A method is described for the rapid production and purification of new potential dopamine agonists. Via microwave heating 10,11-dihydroxy-N-(n-2-fluoroethyl)norapomorphine (FNEA), 10,11-dihydroxy-N-(n-3-fluoropropyl)norapomorphine (FNPA) and 2,10,11-trihydroxy-N-(n-3-fluoropropyl)norapomorphine (FTNPA) and their isotopic fluorine-18 derivatives were synthesized. The fluorine-18 label was introduced via N-fluoroalkylation of acylated noraporphine derivatives with no-carrier-added (n.c.a.) 18FCH2CH2I and 18FCH2CH2CH2I. Within 160 min (E.O.B.), radiochemical yields of 13-29% (corrected for decay) were achieved based on [18F]fluoroalkyliodide. The specific activity obtained, ranged from 15 to 75 GBq/mumol. The fluorine-18 labeled compounds were investigated for their in vivo binding potency to the D2-receptors. After i.v. injection, the distribution was studied in rats. High uptakes of the N-[18F]fluoroalkylaporphines were found in the lungs, liver, adrenals and kidneys. No significant different radioactive accumulation was observed in striatum, cerebellum and frontal cortex. Dopamine depletion with reserpine did not affect the striatum to cerebellum ratio at low dosage of N-[18F]fluoroalkylaporphines (10 nmol/kg).

UI	MeSH Term	Description	Entries
D007553	Isotope Labeling	Techniques for labeling a substance with a stable or radioactive isotope. It is not used for articles involving labeled substances unless the methods of labeling are substantively discussed. Tracers that may be labeled include chemical substances, cells, or microorganisms.	Isotope Labeling, Stable,Isotope-Coded Affinity Tagging,Isotopically-Coded Affinity Tagging,Affinity Tagging, Isotope-Coded,Affinity Tagging, Isotopically-Coded,Isotope Coded Affinity Tagging,Labeling, Isotope,Labeling, Stable Isotope,Stable Isotope Labeling,Tagging, Isotope-Coded Affinity,Tagging, Isotopically-Coded Affinity
D008297	Male		Males
D005462	Fluorine Radioisotopes	Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes.	Radioisotopes, Fluorine
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001058	Apomorphine	A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.	Apokinon,Apomorphin-Teclapharm,Apomorphine Chloride,Apomorphine Hydrochloride,Apomorphine Hydrochloride Anhydrous,Apomorphine Hydrochloride, Anhydrous,Apomorphine Hydrochloride, Hemihydrate,Britaject,Apomorphin Teclapharm
D014018	Tissue Distribution	Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.	Distribution, Tissue,Distributions, Tissue,Tissue Distributions
D015259	Dopamine Agents	Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.	Dopamine Drugs,Dopamine Effect,Dopamine Effects,Dopaminergic Agents,Dopaminergic Drugs,Dopaminergic Effect,Dopaminergic Effects,Agents, Dopamine,Agents, Dopaminergic,Drugs, Dopamine,Drugs, Dopaminergic,Effect, Dopamine,Effect, Dopaminergic,Effects, Dopamine,Effects, Dopaminergic
D017208	Rats, Wistar	A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.	Wistar Rat,Rat, Wistar,Wistar Rats
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus