N-(/sup 11/C)-methyl-p-substituted phentermine analogs as potential brain blood flow agents for positron tomography

Conference · Sat Dec 31 23:00:00 EST 1983 · J. Nucl. Med.; (United States)

OSTI ID:6793554

Kizuka, H; Elmaleh, D R; Boudreaux, G J; Anderton, K D; Strauss, H W; Ackerman, R H; Brownell, G L

The addition of a methyl group to the ..cap alpha..-position of amphetamine increases both the lipophilicity of the agent and its resistance to metabolism by monoamine oxidase. In addition, since tritium substituted phenteramine analog studies suggested that the p-halo phentermines had a greater concentration in the brain and prolonged retention time, the authors evaluated the biological behavior of positron labeled ..cap alpha..-methylamphetamine (phenteramine) in rats, dogs and monkeys. The N-(/sup 11/C) methyl analogs of p-chloro (I) and p-fluoro (II) phentermines were prepared by methylation of their primary amines using /sup 11/Ch/sub 3/I. Biodistribution studies in rats shows brain uptake is in the range of 1% dose/gr at 5 and 15 min for both agents. The activity in blood and eyes is low. Sequential images of the dogs' brain over 1 hour revealed a clearance of <15%. Images of the monkey brain were also obtained using a MGH positron camera PCR-I.

• Research Organization: Massachusetts General Hospital, Boston, MA 02114
• OSTI ID: 6793554
• Report Number(s): CONF-840619-
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:5; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

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59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
ALKYL RADICALS
AMINE OXIDASES
AMPHETAMINES
ANALEPTICS
ANIMALS
ANTILEPTONS
ANTIMATTER
ANTIPARTICLES
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BLOOD FLOW
BODY
BRAIN
CARBON 11
CARBON ISOTOPES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CHEMICAL PREPARATION
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DISTRIBUTION
DOGS
DRUGS
ELEMENTARY PARTICLES
ELEMENTS
EMISSION COMPUTED TOMOGRAPHY
ENZYMES
EVEN-ODD NUCLEI
FERMIONS
HYDROGEN ISOTOPES
IMAGES
ISOTOPES
LABELLING
LEPTONS
LIGHT NUCLEI
MAMMALS
METABOLISM
METHYL RADICALS
MINUTES LIVING RADIOISOTOPES
MONKEYS
NERVOUS SYSTEM
NITROGEN
NONMETALS
NUCLEI
ODD-EVEN NUCLEI
ORGANS
OXIDOREDUCTASES
POSITRON COMPUTED TOMOGRAPHY
POSITRONS
PRIMATES
QUANTITY RATIO
RADICALS
RADIOISOTOPES
RATS
RETENTION
RODENTS
SYMPATHOMIMETICS
SYNTHESIS
TIME DEPENDENCE
TISSUE DISTRIBUTION
TOMOGRAPHY
TRITIUM
VERTEBRATES
YEARS LIVING RADIOISOTOPES