Svoboda | Graniru | BBC Russia | Golosameriki | Facebook

To install click the Add extension button. That's it.

The source code for the WIKI 2 extension is being checked by specialists of the Mozilla Foundation, Google, and Apple. You could also do it yourself at any point in time.

How to transfigure the Wikipedia

Would you like Wikipedia to always look as professional and up-to-date? We have created a browser extension. It will enhance any encyclopedic page you visit with the magic of the WIKI 2 technology.

Try it — you can delete it anytime.

Install in 5 seconds
4,5
Kelly Slayton
Congratulations on this excellent venture… what a great idea!
Alexander Grigorievskiy
I use WIKI 2 every day and almost forgot how the original Wikipedia looks like.
Live Statistics
English Articles
Improved in 24 Hours
Added in 24 Hours
What we do. Every page goes through several hundred of perfecting techniques; in live mode. Quite the same Wikipedia. Just better.
Great Wikipedia has got greater.
.
Leo
Newton
Brights
Milds

Nifene

From Wikipedia, the free encyclopedia

Nifene (18F)
Clinical data
ATC code
  • None
Legal status
Legal status
  • Research compound
Identifiers
  • 3-[(2S)-2,5-Dihydro-1H-pyrrol-2-ylmethoxy]-2-18F-fluoropyridine
CAS Number
Chemical and physical data
FormulaC10H11FN2O
Molar mass194.209 g·mol−1
3D model (JSmol)
  • C1C=C[C@H](N1)COC2=C(N=CC=C2)[18F]
  • InChI=1S/C10H11FN2O/c11-10-9(4-2-6-13-10)14-7-8-3-1-5-12-8/h1-4,6,8,12H,5,7H2/t8-/m0/s1/i11-1
  • Key:GHHQHFNDKOQCRS-IZFLLFDKSA-N

Nifene is a high affinity, selective nicotinic α4β2* receptor partial agonist used in medical research for nicotinic acetylcholine receptors, usually in the form of nifene (18F)[1][2] as a positron emission tomography (PET) radiotracer.[3][4]

Nifene has been used to assess the efficacy of acetylcholinesterase inhibitors in animal models, because the neurotransmitter acetylcholine competes with the binding of nifene at the nicotinic receptor site.[5][6] Learning and behavior studies in animal models using nifene have suggested a potential role of the nicotinic receptors located in distinct white matter tracts.[7] Nifene studies in animal models of lung cancer have suggested an upregulation of the nicotinic receptor in the lung tumors.[8][9] Novel PET and SPECT imaging agents as potential receptor antagonists have been developed based on the structure of nifene; niodene for SPECT,[10] nifrolene for PET [11] and niofene for PET/SPECT.[12] These new derivatives take advantage of the unique in vivo imaging properties of nifene.[13] Human studies with (18F)-nifene make it a promising nicotinic α4β2* receptor PET radiotracer for scientific research and has exhibited reliable test-retest reproducibility.[14] Human white matter thalamic radiations (or tracts) were well demarcated and quantified using (18F)-nifene.[15]

References

  1. ^ Pichika R, Easwaramoorthy B, Collins D, Christian BT, Shi B, Narayanan TK, et al. (April 2006). "Nicotinic alpha4beta2 receptor imaging agents: part II. Synthesis and biological evaluation of 2-[18F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine (18F-nifene) in rodents and imaging by PET in nonhuman primate". Nuclear Medicine and Biology. 33 (3): 295–304. doi:10.1016/j.nucmedbio.2005.12.017. PMID 16631077.
  2. ^ Leung K (2004). "2-18FFluoro-3-2-((S)-3-pyrrolinyl)methoxypyridine". PMID 20641387. {{cite journal}}: Cite journal requires |journal= (help)
  3. ^ Kant R, Constantinescu CC, Parekh P, Pandey SK, Pan ML, Easwaramoorthy B, Mukherjee J (June 2011). "Evaluation of F-nifene binding to α4β2 nicotinic receptors in the rat brain using microPET imaging". EJNMMI Research. 1: 6. doi:10.1186/2191-219X-1-6. PMC 3203019. PMID 22039577.
  4. ^ Hillmer AT, Wooten DW, Slesarev MS, Ahlers EO, Barnhart TE, Murali D, et al. (September 2012). "PET imaging of α4β2* nicotinic acetylcholine receptors: quantitative analysis of 18F-nifene kinetics in the nonhuman primate". Journal of Nuclear Medicine. 53 (9): 1471–80. doi:10.2967/jnumed.112.103846. PMC 3580212. PMID 22851633.
  5. ^ Easwaramoorthy B, Pichika R, Collins D, Potkin SG, Leslie FM, Mukherjee J (January 2007). "Effect of acetylcholinesterase inhibitors on the binding of nicotinic alpha4beta2 receptor PET radiotracer, (18)F-nifene: A measure of acetylcholine competition". Synapse. 61 (1): 29–36. doi:10.1002/syn.20338. PMID 17068780. S2CID 85303757.
  6. ^ Hillmer AT, Wooten DW, Farhoud M, Higgins AT, Lao PJ, Barnhart TE, et al. (December 2013). "PET imaging of acetylcholinesterase inhibitor-induced effects on α4β2 nicotinic acetylcholine receptor binding". Synapse. 67 (12): 882–6. doi:10.1002/syn.21698. PMC 3806056. PMID 23913347.
  7. ^ Bieszczad KM, Kant R, Constantinescu CC, Pandey SK, Kawai HD, Metherate R, et al. (May 2012). "Nicotinic acetylcholine receptors in rat forebrain that bind 18F-nifene: relating PET imaging, autoradiography, and behavior". Synapse. 66 (5): 418–34. doi:10.1002/syn.21530. PMC 3292694. PMID 22213342.
  8. ^ Galitovskiy V, Kuruvilla SA, Sevriokov E, Corches A, Pan ML, Kalantari-Dehaghi M, et al. (June 2013). "18F-Nifene PET/CT using A/J mice treated with NNK". Journal of Cancer Research & Therapy. 1 (4): 128–137. doi:10.14312/2052-4994.2013-20. PMC 5443253. PMID 28553544.
  9. ^ Tang W, Kuruvilla SA, Galitovskiy V, Pan ML, Grando SA, Mukherjee J (2014). "Targeting histone deacetylase in lung cancer for early diagnosis: (18)F-FAHA PET/CT imaging of NNK-treated A/J mice model". American Journal of Nuclear Medicine and Molecular Imaging. 4 (4): 324–32. PMC 4074498. PMID 24982818.
  10. ^ Pandey SK, Pan S, Kant R, Kuruvilla SA, Pan ML, Mukherjee J (December 2012). "Synthesis and evaluation of 3-123I-iodo-5-[2-(S)-3-pyrrolinylmethoxy]-pyridine (niodene) as a potential nicotinic α4β2 receptor imaging agent". Bioorganic & Medicinal Chemistry Letters. 22 (24): 7610–4. doi:10.1016/j.bmcl.2012.10.012. PMC 3508149. PMID 23116890.
  11. ^ Pichika R, Kuruvilla SA, Patel N, Vu K, Sinha S, Easwaramoorthy B, et al. (January 2013). "Nicotinic α4β2 receptor imaging agents. Part IV. Synthesis and biological evaluation of 3-(2-(S)-3,4-dehydropyrrolinyl methoxy)-5-(3'-18F-fluoropropyl)pyridine (18F-Nifrolene) using PET". Nuclear Medicine and Biology. 40 (1): 117–25. doi:10.1016/j.nucmedbio.2012.09.009. PMC 3514651. PMID 23141552.
  12. ^ Kuruvilla SA, Hillmer AT, Wooten DW, Patel A, Christian BT, Mukherjee J (2014). "Synthesis and evaluation of 2-(18)F-fluoro-5-iodo-3-[2-(S)-3,4-dehydropyrrolinylmethoxy]pyridine ((18)F-Niofene) as a potential imaging agent for nicotinic α4β2 receptors". American Journal of Nuclear Medicine and Molecular Imaging. 4 (4): 354–64. PMC 4074501. PMID 24982821.
  13. ^ Hillmer AT, Wooten DW, Slesarev MS, Ahlers EO, Barnhart TE, Schneider ML, et al. (November 2013). "Measuring α4β2* nicotinic acetylcholine receptor density in vivo with [(18)F]nifene PET in the nonhuman primate". Journal of Cerebral Blood Flow and Metabolism. 33 (11): 1806–14. doi:10.1038/jcbfm.2013.136. PMC 3824181. PMID 23942367.
  14. ^ Lao PJ, Betthauser TJ, Tudorascu DL, Barnhart TE, Hillmer AT, Stone CK, Mukherjee J, Christian BT (August 2017). "[18 F]Nifene test-retest reproducibility in first-in-human imaging of α4β2* nicotinic acetylcholine receptors". Synapse. 71 (8). New York, N.Y.: e21981. doi:10.1002/syn.21981. PMC 5541262. PMID 28420041.
  15. ^ Mukherjee J, Lao PJ, Betthauser TJ, Samra GK, Pan ML, Patel IH, Liang C, Metherate R, Christian BT (January 2018). "Human brain imaging of nicotinic acetylcholine α4β2* receptors using [18 F]Nifene: Selectivity, functional activity, toxicity, aging effects, gender effects, and extrathalamic pathways". The Journal of Comparative Neurology. 526 (1): 80–95. doi:10.1002/cne.24320. PMC 5788574. PMID 28875553.

External links


Stub icon

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

This page was last edited on 24 April 2024, at 19:51
Basis of this page is in Wikipedia. Text is available under the CC BY-SA 3.0 Unported License. Non-text media are available under their specified licenses. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc. WIKI 2 is an independent company and has no affiliation with Wikimedia Foundation.
Contact WIKI 2
Introduction
Terms of Service
Privacy Policy