8-AZABICYCLO[3.2.1]OCTANE-2-CARBOXYLIC ACID, 8-(3-FLUOROPROPYL)-3-(4-IODOPHENYL)-, METHYL ESTER (1R,2S,3S,5S)-

Absorption

Absorption is 100% because administered I.V.

Description

loflupane was launched as a new imaging agent for investigation of the dopaminergic neurons and the early diagnosis of Parkinson’s disease and related syndromes. This (¹²³I) iodine-labeled agent was developed for imaging with single-photon emission computed tomography (SPECT); it binds to dopamine transporters on cerebral neurons, enabling the detection of an eventual loss of functional neurons, particularly in the striatal region. The use in clinical routine of SPECT technique with this new agent generates reliable and reproducible results in healthy control subjects as well as in patients with Parkinson’s disease. So, it displays a quantification of striatal dopaminergic function and can help in the identification of the parkinsonian syndromes and their differentiation from syndromes due to other diseases. The major metabolic reactions in healthy humans are hydrolysis of the ester bond to the free acid and N-dealkylation to the ¹²³-I labeled noranalog.

Originator

Research Biochemicals Int (UK)

Indications

Ioflupane I-123 is a SPECT (single photon emission computerized tomography) agent used to distinguish between Parkinson’s syndrome tremors and essential tremor.

Background

Ioflupane (I-123) is a radiopharmaceutical used to image dopamine neurons and diagnose Parkinsonian syndromes.

Definition

ChEBI: An azabicycloalkane that is ecgonine methyl ester in which the N-methyl group is replaced by 3-fluoropropyl and the 3beta-hydroxy group is replaced by 4-(123I)iodophenyl. Used for the imaging of dopa ine transporters in the brain of adult patients with potential Parkinsonian Syndromes.

brand name

DatSCAN

Pharmacokinetics

iodine-123 labeled ioflupanebinds selectively to striatal presynaptic dopamine neurons by binding reversibly to presynaptic dopamine transporters.

Metabolism

Not Available