Preparation and biodistribution of 1-(2-(3-(/sup 125/I)iodo-4-aminophenyl)ethyl)-4-(3-(trifluoromethyl) phenyl)piperazine and 1-(2-(3-(/sup 125/I)iodo-4-azidophenyl)ethyl)-4-(3-(trifluoromethyl)phenyl) piperazine
The iodinated analogue of 1-(2-(4-aminophenyl)ethyl)-4-(3-(trifluoromethyl)phenyl)piperazine (PAPP), IPAPP (4), and the corresponding azido compound azido-IPAPP (5) were synthesized. The corresponding no-carrier-added /sup 125/I (T1/2 = 60 days, 35-60 keV) labeled compounds were also prepared. High specific binding was observed from in vitro binding studies using rat brain tissue preparation; Ki = 20 and 17.5 nM against (/sup 3/H)-5-HT. In vivo biodistribution studies in rats showed that azido-(/sup 125/I)IPAPP passed through intact blood-brain barrier and localized in the brain. Ex vivo autoradiography of rat brain sections exhibited a diffuse uptake pattern, which may be due to specific and nonspecific binding. The results indicate that IPAPP and azido-IPAPP may not be suitable to image the serotonin receptor in the brain.
- Research Organization:
- Univ. of Pennsylvania, Philadelphia (USA)
- OSTI ID:
- 6075270
- Journal Information:
- J. Med. Chem.; (United States), Vol. 32:3
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
TISSUE DISTRIBUTION
AUTORADIOGRAPHY
AZIDES
BIOCHEMICAL REACTION KINETICS
BLOOD-BRAIN BARRIER
BRAIN
CATTLE
IN VITRO
IODINE 125
PIPERAZINES
RATS
SEROTONIN
TRITIUM COMPOUNDS
AMINES
ANIMALS
AROMATICS
AUTONOMIC NERVOUS SYSTEM AGENTS
AZAARENES
AZINES
AZOLES
BETA DECAY RADIOISOTOPES
BODY
CENTRAL NERVOUS SYSTEM
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DOMESTIC ANIMALS
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
HETEROCYCLIC COMPOUNDS
HYDROXY COMPOUNDS
INDOLES
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOTOPES
KINETICS
LABELLED COMPOUNDS
MAMMALS
NERVOUS SYSTEM
NEUROREGULATORS
NITROGEN COMPOUNDS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PYRAZINES
PYRROLES
RADIOISOTOPES
RADIOPROTECTIVE SUBSTANCES
REACTION KINETICS
RODENTS
RUMINANTS
SYMPATHOMIMETICS
SYNTHESIS
TRYPTAMINES
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics