Ioflupane I-123 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
iodine-containing contrast media	4230	155798-07-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: Ioflupane I 123 DaTSCAN Ioflupane I-123 Ioflupane (123I)	Ioflupane binds reversibly to the human recombinant dopamine transporter (DaT). Following administration of DaTscan to humans, radioactive decay of the iodine 123 emits gamma radiation which can be detected externally using gamma detectors, allowing visualization of the brain striata through SPECT imaging. Autoradiography of post-mortem human brain slices exposed to radiolabeled ioflupane shows concentration of the radiolabel in striatum (caudate nucleus and putamen). The specificity of the binding of ioflupane I 125 to dopamine transporter was demonstrated by competition studies with the DaT inhibitor GBR 12909 (a dopamine reuptake inhibitor), the serotonin reuptake inhibitor citalopram, and the norepinephrine reuptake inhibitor desipramine in post-mortem human brain slices exposed to radiolabeled ioflupane. Citalopram reduced binding in the neocortex and thalamus with only minor effects in the striatum. This indicated that the binding in the cortex and thalamus is mainly to the serotonin reuptake sites. Desipramine showed no effect on the level of striatal binding of ioflupane I 125, but reduced extrastriatal binding by 60 to 85%. The binding of ioflupane I 125 to the striatum was abolished in the presence of high concentrations of GBR 12909, indicating selectivity of ioflupane binding for the pre-synaptic DaT. Molecular weight: 427.29 Formula: C18H23FINO2 CLOGP: 4.42 LIPINSKI: 0 HAC: 3 HDO: 0 TPSA: 29.54 ALOGS: -4.88 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

Ioflupane I 123
DaTSCAN
Ioflupane I-123
Ioflupane (123I)

Ioflupane binds reversibly to the human recombinant dopamine transporter (DaT). Following administration of DaTscan to humans, radioactive decay of the iodine 123 emits gamma radiation which can be detected externally using gamma detectors, allowing visualization of the brain striata through SPECT imaging. Autoradiography of post-mortem human brain slices exposed to radiolabeled ioflupane shows concentration of the radiolabel in striatum (caudate nucleus and putamen). The specificity of the binding of ioflupane I 125 to dopamine transporter was demonstrated by competition studies with the DaT inhibitor GBR 12909 (a dopamine reuptake inhibitor), the serotonin reuptake inhibitor citalopram, and the norepinephrine reuptake inhibitor desipramine in post-mortem human brain slices exposed to radiolabeled ioflupane. Citalopram reduced binding in the neocortex and thalamus with only minor effects in the striatum. This indicated that the binding in the cortex and thalamus is mainly to the serotonin reuptake sites. Desipramine showed no effect on the level of striatal binding of ioflupane I 125, but reduced extrastriatal binding by 60 to 85%. The binding of ioflupane I 125 to the striatum was abolished in the presence of high concentrations of GBR 12909, indicating selectivity of ioflupane binding for the pre-synaptic DaT.

Molecular weight: 427.29
Formula: C18H23FINO2
CLOGP: 4.42
LIPINSKI: 0
HAC: 3
HDO: 0
TPSA: 29.54
ALOGS: -4.88
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
June 25, 2019	EMA	CIS bio international
Jan. 14, 2011	FDA	GE HLTHCARE INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
FDA MoA	N0000000205	Radiopharmaceutical Activity
FDA EPC	N0000177914	Radioactive Diagnostic Agent
CHEBI has role	CHEBI:35232	radiopharmaceuticals

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Striatal dopamine transporter visualization using single photon emission computed tomography	indication	105371005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.9	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	BINDING AGENT	Ki	9.21		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
4030845	VUID
N0000182831	NUI
4030845	VANDF
C1956796	UMLSCUI
CHEBI:68855	CHEBI
CHEMBL3989517	ChEMBL_ID
DB08824	DRUGBANK_ID
7500	INN_ID
3MM99T8R5Q	UNII
3086674	PUBCHEM_CID
1426874	RXNORM
179428	MMSL
22309	MMSL
d05895	MMSL
013745	NDDF
428122004	SNOMEDCT_US
429296007	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
DaTscan	HUMAN PRESCRIPTION DRUG LABEL	1	17156-210	INJECTION, SOLUTION	2 mCi	INTRAVENOUS	NDA	31 sections
DaTscan	HUMAN PRESCRIPTION DRUG LABEL	1	17156-210	INJECTION, SOLUTION	2 mCi	INTRAVENOUS	NDA	31 sections
DaTscan	HUMAN PRESCRIPTION DRUG LABEL	1	17156-210	INJECTION, SOLUTION	2 mCi	INTRAVENOUS	NDA	31 sections
Ioflupane I 123	HUMAN PRESCRIPTION DRUG LABEL	1	69945-166	INJECTION, SOLUTION	2 mCi	INTRAVENOUS	ANDA	29 sections
Ioflupane I 123	HUMAN PRESCRIPTION DRUG LABEL	1	69945-166	INJECTION, SOLUTION	2 mCi	INTRAVENOUS	ANDA	29 sections