18F-SDM-8 material

¹⁸F- SDM -8 Materials

1.  Drug Name (Generic Name, Chemical Name, English Name, Pinyin, and rationale for custom n≠ames if any)

Generic Name: 18F- SDM -8

Chemical Name: (R)-4-(3 - fluoro - 5-( fluoro - 18F) phenyl )-1-((3 - methylpyridine - 4 - yl ) methyl ) pyrrolidine - 2 - one  

English Name: (R)-4-(3-Fluoro-5-(fluorine-18F) phenyl)-1-((3-methylpyridin-4-yl) methyl) pyrrolidin-2-'one

Pinyin: (R)-4-(3-fú - 5-(fú - 18F)běn jī)-1-((3-jiǎ jī bǐ dìng - 4-jī)jiǎ jī)bǐλ luò wán - 2-tóng

2. Drug Chemical Structure, Molecular Weight, Molecularπ Formula

Chemical Structure:

Molecular Weight: 317 

Molecular Formula: C ₁₈ H ₁₉ F ₂​ N ₂​ O _​

3. Rationale ( Literature on the research and application of this product at home and abroad¥ )

Research and Application Abroad

• Research: Abroad, 18F-SDM-8 is being researched as a novel positron emission tomo♦graphy (PET) radiotracer. Related synthesis and in vivo evaluation studies have shown &that its in vitro binding test shows high binding affinity for synaptiαc vesicle glycoprotein 2A (SV2A) (Ki = 0.58 nM), with hig♦h molar activity (241.7 MBq/nmol) and high radiochemical purity (>98%) <during preparation. In rhesus monkey brain studies, it showed high uptake, with p‍eak standardized uptake values (SUV) greater than 8, ‍and rapid reversible kinetic characteristics. Through displac♣ement and blockade studies with levetiracetam, 11C-UCB-J, etc., the reversibiliβty and specificity of its binding to SV2A were confirmed.
• Application: Mainly focuses on neurodegenerative and mental i≤llnesses. Because it can target SV2A, and synaptic structure damage and ch​anges are related to many brain diseases, such as βAlzheimer's disease, epilepsy, depression, and schizophrenia, 18F-SDM-8↔ is expected to become a biomarker for measuring synaptic density, ↑assisting in the diagnosis and assessment of these diseases. At the same time, in multimod≈al imaging studies, it is used in combination with other tracers (such as  18F-FDG) to explore the spatiotemporal relationship ≥between different neuropathological events to eluci§date the pathological process of neurodegenerative diseases.

Research and Application in China

• Research: There are also relevant research explorations on 18F-SDM-8 in China. I←mprovements may be made in the synthesis process to meet the quality and qu‌antity requirements of preclinical research and future clinical applicati×ons.
• Application: Studies have used 18F-SDM-8 for imaging of a rat temporal lobe epilepsy ÷model. By performing 18F-SDM-8 and 18F-FDG microPET/CT imag<ing at different time points (acute phase, latent phase, chronic phaσse) in rats with epilepsy induced by alginate injection, the asymmetry index ≠(AI) was calculated to evaluate its ability to identify epileptic foci. The results §showed that there was a statistically significant difference in the AI of the hippocamβpus between the epilepsy group and the control group in imaging ♥at different time points, and the imaging agent shoπwed asymmetrical uptake in the epilepsy group, consistent with the ↑pathological staining results, showing its application potential in the dete¶ction of epileptic foci.

4 Research methods, experimental conditions, etc., of imaging or simulated clinical funct ional determination tests of target organs and the whole body of experimental animals, and" imaging or functional determination results at various time phases

[Drug Name]

Generic Name: 18F-SDM-8

Chemical Name: (4R)-4-(3-(¹⁸F)fluoranyl-5-fluorophenyl)-1-[(3-methylpyridin-4-yl)methyl]pyrrolidin- 2-one

English Name: 18F-Sdm-8

Pinyin: shíbā F-S-D-M-bā

[Ingredients]

The main component and its chemical name are: Synaptic Vesic¶le Glycoprotein 2A (SV2A)

Its structural formula is:

[Properties]

This product is a colorless or slightly yellow, clear liquid.

Indications: Epilepsy focus localization; lesion detection in focal cortical dysplasia ₩(FCD); synaptic density assessment in central neurodegenerative disea$ses; other neurological disease research.

18F-Sdm-8 PET/CT Brain Imaging Procedure

I. Pre-examination Preparation

Diet and medication management:

Avoid strenuous exercise within 24 hours before the examination, and fast for 4-6 hours (¶water is allowed) to reduce blood glucose interference.

Diabetic patients need to control their blood glucose in advance (fasting blood glucose is recom‍mended to be ≤11 mmol/L), and adjust the time of hypoglycemic medication if necessaβry.

Medical history collection and contraindication sc reening:

Provide previous imaging reports (such as MRI, CT), pathol£ogy results, and medication records.

Confirm that there is no claustrophobia, severe pain, or agitation that would preven♠t cooperation with the examination.

Environmental and clothing requirements:

Change into clothing without metal ornaments before the examinat ion, and remove dentures, hair clips, and other interfering objects.

Keep the environment warm to avoid cold stimulation causing brown fat to uptake tγhe imaging agent.

II. Radiopharmaceutical Injection and Rest Period

Drug injection:

Intravenous injection of 18F-SDM-8 (dosage adjusted according to∏ weight and equipment requirements), remain seated or supine after i✘njection.

Resting wait:

After injection, rest for 45-60 minutes in a dark, quiet environment, avoid ta←lking, chewing, or mental activity to ensure that the imaging agent is evenly distributed inφ the brain.

Drink plenty of water to promote the metabolism of the imaging agent, and empty the bladder b‌efore the examination.

PET/CT acquisition: Scanning should be performed o≠n time 50 minutes after injection of the imaging agent. St₩atic scanning time is 50 minutes after injection, and a≈cquisition is 20 minutes. Dynamic acquisition time is 0-70 minutes. CT and PE☆T acquisition parameters and reconstruction methods should be consistent with brain 1±8F-FDG imaging. The scanning group needs to strictly control the inj‌ection time and scanning time, and strictly record the scanning time.

Image interpretation and analysis: Interpret images promptly.

Report: Issue a report promptly.

Follow-up arrangements: 18F-Sdm-8 and 18F-FDG brain imagin₽g should be spaced at least 10 half-lives (or 20 hours) apart.

This product can only be used in medical institutions< with a "Radioactive Pharmaceutical Use License".

Adverse Reactions

None found.

Contraindications

None found.

Precautions

If discoloration or turbidity occurs, discontinue use.

This product can only be used in medical institutions with a "Radioactive Pharmaceutica♦l Use License".

Use in Pregnant and Lactating Women

Contraindicated in pregnant and lactating women.

Pediatric Use

Reduce dosage appropriately according to weight.

Specifications

0.37~7.40GBq.

Storage and Packaging

This product is sealed in a 30ml vial and placed in a lead contain©er.

Shelf Life

6 hours from the calibration time.

Manufacturer

Name: Hangzhou Jirei Technology Co., Ltd.

Address: No. 319, Shenjia Road, Gongshu District, Hangzhou, Fengqi Valley Y'unzhang Industrial Park

Postal Code: 234122

Telephone Number: 0571-87701916