Screening models for CNS activity – anti-inflammatory drugs explores experimental approaches used to identify and validate compounds that reduce neuroinflammation. This introduction covers in vivo and in vitro models, behavioral and biochemical endpoints, biomarkers such as cytokines, Iba1, GFAP, and imaging targets like TSPO, plus blood‑brain barrier and pharmacokinetic considerations. B. Pharm students should grasp practical assays (Griess, ELISA, qPCR, Western blot), cell lines (BV2, hCMEC/D3), and animal models (LPS, EAE, MPTP, APP/PS1) used in preclinical screening. Emphasis is on selecting appropriate models, interpreting biomarkers, and integrating PK/PD for CNS penetration. Now let’s test your knowledge with 30 MCQs on this topic.
Q1. What is the primary experimental purpose of screening models for CNS activity in anti-inflammatory drug development?
- To evaluate a compound’s ability to modulate neuroinflammation, molecular markers and relevant behaviors
- To determine only the compound’s hepatic metabolism rates
- To replace clinical trials with animal data
- To assess taste and color of the formulation
Correct Answer: To evaluate a compound’s ability to modulate neuroinflammation, molecular markers and relevant behaviors
Q2. Which in vivo model is most commonly used for acute neuroinflammation screening of anti-inflammatory agents?
- Lipopolysaccharide (LPS)-induced neuroinflammation in rodents
- Complete Freund’s adjuvant-induced arthritis
- Dextran sulfate sodium-induced colitis
- Zebrafish fin regeneration assay
Correct Answer: Lipopolysaccharide (LPS)-induced neuroinflammation in rodents
Q3. Which microglial cell line is widely used for in vitro screening of anti-inflammatory activity in CNS research?
- BV2 murine microglial cell line
- HEK293 kidney cell line
- CHO ovary cell line
- RAW 264.7 macrophage cell line
Correct Answer: BV2 murine microglial cell line
Q4. Which protein is a common immunohistochemical marker of microglial activation?
- Iba1 (ionized calcium-binding adaptor molecule 1)
- GFAP (glial fibrillary acidic protein)
- NeuN (neuronal nuclei)
- Albumin
Correct Answer: Iba1 (ionized calcium-binding adaptor molecule 1)
Q5. Which marker is most commonly used to detect astrocyte activation in neuroinflammation studies?
- GFAP (glial fibrillary acidic protein)
- Caspase-3
- Myelin basic protein
- CD31
Correct Answer: GFAP (glial fibrillary acidic protein)
Q6. Which cytokine is typically measured as an early pro‑inflammatory mediator in CNS inflammation models?
- IL-1β
- IL-10
- Transforming growth factor-beta (TGF-β)
- Adiponectin
Correct Answer: IL-1β
Q7. Which enzymatic product is commonly measured to assess COX-2–mediated inflammation in CNS studies?
- PGE2 (prostaglandin E2)
- Dopamine
- Glutathione
- Serotonin
Correct Answer: PGE2 (prostaglandin E2)
Q8. Which assay is standard for quantifying nitrite as an indirect measure of nitric oxide release in cell culture?
- Griess assay
- Comet assay
- Bradford protein assay
- Alamar Blue assay
Correct Answer: Griess assay
Q9. Which dye is classically used to assess blood–brain barrier (BBB) permeability in animal models?
- Evans blue
- Crystal violet
- Trypan blue
- Rhodamine 123
Correct Answer: Evans blue
Q10. Which PET imaging target is widely used as a biomarker of microglial activation and neuroinflammation?
- TSPO (translocator protein)
- NMDA receptor
- Acetylcholinesterase
- Monoamine oxidase A
Correct Answer: TSPO (translocator protein)
Q11. Which animal model is commonly used to study neuroinflammatory mechanisms of multiple sclerosis?
- Experimental autoimmune encephalomyelitis (EAE)
- MPTP-induced Parkinsonism
- Lewis lung carcinoma model
- Adriamycin cardiotoxicity model
Correct Answer: Experimental autoimmune encephalomyelitis (EAE)
Q12. Which neurotoxin is used to create a rodent model of Parkinson’s disease for testing anti-inflammatory neuroprotective drugs?
- MPTP
- Kainic acid
- LPS
- Rotenone
Correct Answer: MPTP
Q13. Which agent is used to induce excitotoxic neuronal injury and neuroinflammation in seizure and injury models?
- Kainic acid
- Streptozotocin
- Isoproterenol
- Alloxan
Correct Answer: Kainic acid
Q14. What is a major advantage of organotypic brain slice cultures for screening CNS anti-inflammatory drugs?
- They preserve native cytoarchitecture and cell–cell interactions
- They are identical to in vivo pharmacokinetics
- They eliminate the need for biochemical assays
- They cannot be used for imaging studies
Correct Answer: They preserve native cytoarchitecture and cell–cell interactions
Q15. Which behavioral test is commonly used to detect depressive‑like effects that may relate to neuroinflammation?
- Forced swim test
- Morris water maze reversal test
- Grip strength test
- Hot plate test
Correct Answer: Forced swim test
Q16. Which behavioral assay assesses motor coordination and is useful in neuroinflammatory or neurodegenerative screening?
- Rotarod performance test
- Tail flick test
- Open field center time
- Elevated plus maze
Correct Answer: Rotarod performance test
Q17. Which technique is standard for quantifying mRNA levels of inflammatory mediators in CNS tissue?
- qPCR (quantitative real-time PCR)
- Mass spectrometry proteomics
- Flow cytometry of live blood cells
- Patch‑clamp electrophysiology
Correct Answer: qPCR (quantitative real-time PCR)
Q18. Which method measures specific protein expression changes (e.g., iNOS, COX-2) in brain homogenates?
- Western blotting
- GC–MS of volatile compounds
- In vivo microdialysis without analysis
- Electroencephalography (EEG)
Correct Answer: Western blotting
Q19. Which assay is most appropriate to quantify cytokine protein levels in brain tissue or culture supernatant?
- ELISA (enzyme-linked immunosorbent assay)
- Gram staining
- Hematoxylin and eosin staining
- Western blot without antibodies
Correct Answer: ELISA (enzyme-linked immunosorbent assay)
Q20. Which pharmacokinetic parameter is most directly used to assess CNS penetration of a drug during preclinical screening?
- Brain-to-plasma concentration ratio
- Urine elimination half-life
- Skin permeability coefficient
- Gastric pH stability
Correct Answer: Brain-to-plasma concentration ratio
Q21. Which in silico metric is commonly used to predict a molecule’s likelihood to reach the CNS?
- CNS MPO (multiparameter optimization) score
- CYP450 inhibition constant only
- MIC (minimum inhibitory concentration)
- Separation factor (Rs) in HPLC
Correct Answer: CNS MPO (multiparameter optimization) score
Q22. Increased binding of TSPO PET ligands in a brain region typically indicates:
- Microglial activation and neuroinflammation
- Increased synaptic transmission only
- Loss of myelin with no inflammation
- Enhanced blood flow without immune involvement
Correct Answer: Microglial activation and neuroinflammation
Q23. Which neuronal marker is often used to quantify neuronal loss in histological sections?
- NeuN
- GFAP
- Iba1
- CD68
Correct Answer: NeuN
Q24. Which transgenic mouse model is widely used to study chronic neuroinflammation relevant to Alzheimer’s disease?
- APP/PS1 double-transgenic mice
- NOD scid mice for immunodeficiency
- db/db diabetic mice
- shiverer myelin-deficient mice
Correct Answer: APP/PS1 double-transgenic mice
Q25. Which biochemical assay is commonly used to assess lipid peroxidation as a marker of oxidative stress in CNS tissue?
- MDA (malondialdehyde) assay
- Urea assay
- Alkaline phosphatase activity
- Creatinine clearance
Correct Answer: MDA (malondialdehyde) assay
Q26. Which method is typically used to quantify PGE2 levels in brain homogenates?
- PGE2-specific ELISA
- Hematoxylin staining
- Luciferase reporter assay for promoters
- Ninhydrin assay
Correct Answer: PGE2-specific ELISA
Q27. What is the most important control group when testing an anti-inflammatory candidate in an animal neuroinflammation study?
- Vehicle-treated control group with the same procedure
- An unrelated drug-treated group with different dosing
- No handling and no injection group only
- Only in vitro controls without animals
Correct Answer: Vehicle-treated control group with the same procedure
Q28. After systemic LPS administration, at what time window do many pro‑inflammatory cytokines peak in rodent brains for acute screening?
- 4–6 hours
- 1–2 weeks
- 10–12 days
- Immediately within seconds
Correct Answer: 4–6 hours
Q29. Which inducible enzyme is a major contributor to reactive nitrogen species during neuroinflammation?
- iNOS (inducible nitric oxide synthase)
- Acetylcholinesterase
- Citrate synthase
- DNA polymerase
Correct Answer: iNOS (inducible nitric oxide synthase)
Q30. Which human brain endothelial cell line is commonly used to model the BBB in vitro for permeability and inflammatory studies?
- hCMEC/D3 human brain microvascular endothelial cell line
- MCF-7 breast cancer cell line
- 293T embryonic kidney cell line
- Jurkat T lymphocyte cell line
Correct Answer: hCMEC/D3 human brain microvascular endothelial cell line
I am a Registered Pharmacist under the Pharmacy Act, 1948, and the founder of PharmacyFreak.com. I hold a Bachelor of Pharmacy degree from Rungta College of Pharmaceutical Science and Research. With a strong academic foundation and practical knowledge, I am committed to providing accurate, easy-to-understand content to support pharmacy students and professionals. My aim is to make complex pharmaceutical concepts accessible and useful for real-world application.
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