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Volumn 22, Issue 18, 2012, Pages 5795-5800

Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein - Potential novel positron emitting tomography imaging agents

Author keywords

Neuroinflammation; PBR; PET; Synthesis; TSPO

Indexed keywords

ANILIDE; BENZODIAZEPINE RECEPTOR; DAA 1106; DIARYL ANILIDE; FE DAA 1106; FE PPA; FLUORINE 18; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; NUCLEAR MAGNETIC RESONANCE IMAGING AGENT; PBR 06; PBR 28; TRANSLOCATOR PROTEIN; UNCLASSIFIED DRUG;

EID: 84865499184     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.07.093     Document Type: Article
Times cited : (12)

References (15)
  • 12
    • 84856212426 scopus 로고    scopus 로고
    • Wadsworth, H.; Jones, P.A.; Chau, W.; Durrant, C.; Fouladi, N.; Passmore, J.; O'Shea, D.; Wynn, D.; Morisson-Iveson, V.; Ewan, A.; Thaning, M.; Mantzilas, D.; Gausemel, I.; Khan, I.; Black, A.; Avory, M.; Trigg, W. Bioorg. Med. Chem. Lett. 2012, 22, 1308.Male Wistar rats (200-300 g, 3 per time-point) were intravenously injected test compound (approximately 1-3 MBq at 10 MBq/mL - volume less than 5 mL/Kg, formulated <10% Ethanol in phosphate buffered saline) under anaesthesia (4% isoflurane). At 2, 10, 30 or 60 min post-injection animals were sacrificed by cervical dislocation under anaesthesia. Animals for either humanely restrained or kept in short term metabolism cages to allow for collection of faeces and urine. Blood, bone (whole femur, tibia and fibula from both hind legs), muscle (from both hind legs), skin sample, fat sample, faeces, whole organs/tissues (kidneys, bladder (including urine and voided urine), lung, liver, spleen, stomach (including contents), small and large intestine (including contents), heart, adrenals), injection site (whole tail) and remaining carcass were assessed for radioactivity by a gamma counter. The brain was dissected into striatum, cerebellum, hippocampus, pre-frontal cortex, remaining cortex, pons and medulla, thalamus, olfactory bulbs, hypothalamus and remaining brain and activity determined by a gamma counter. Whole body and regional brain biodistribution was generated. All animal studies were performed in accordance with the Animals (Scientific Procedures) Act 1986 act.
    • (2012) Bioorg. Med. Chem. Lett. , vol.22 , pp. 1308
    • Wadsworth, H.1    Jones, P.A.2    Chau, W.3    Durrant, C.4    Fouladi, N.5    Passmore, J.6    O'Shea, D.7    Wynn, D.8    Morisson-Iveson, V.9    Ewan, A.10    Thaning, M.11    Mantzilas, D.12    Gausemel, I.13    Khan, I.14    Black, A.15    Avory, M.16    Trigg, W.17


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.