Levokabastin

Levokabastin
(IUPAC) ime
	(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
Klinički podaci
Identifikatori
CAS broj	79516-68-0
ATC kod	R01AC02 S01GX02
PubChem	54385
DrugBank	APRD01069
ChemSpider	16736421
UNII	H68BP06S81
KEGG	D08117
ChEMBL	CHEMBL1201312
Hemijski podaci
Formula	C26H29FN2O2
Mol. masa	420.519 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C26H29FN2O2/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20/h2-10,19,23H,11-17H2,1H3,(H,30,31)/t19-,23-,25-,26-/m1/s1 ; Key: ZCGOMHNNNFPNMX-KYTRFIICSA-N
Farmakokinetički podaci
Poluvreme eliminacije	3
Farmakoinformacioni podaci
Trudnoća	B3(AU) C(US)
Pravni status	℞ Prescription only
Način primene	Oftalmično, intranazalno

Levokabastin je selektivni antagonist H₁ receptora druge generacije koji je razvila kompanija Jansen Farmaceutikal 1979. On se koristi za lečenje alergijskog konjunktivitisa.^[7]

Pored antihistaminskog dejstva, levokabastin takođe deluje kao potentan i selektivan antagonist neurotenzinskog receptora NTS₂, i bio je prvi lek koji je korišten za karakterisanje raznih neurotenzinskih podtipova.^[8]^[9]^[10]^[11]^[12]^[13]^[14]

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ „RxMed: Pharmaceutical Information - LIVOSTIN NASAL SPRAY”. Pristupljeno 13 November 2005.
↑ Pipkorn U, Bende M, Hedner J, Hedner T., A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis. Allergy. 1985 Oct;40(7):491-6.
↑ Schotte A, Leysen JE, Laduron PM (August 1986). „Evidence for a displaceable non-specific [3Hneurotensin binding site in rat brain”]. Naunyn-Schmiedeberg's Archives of Pharmacology 333 (4): 400–5. DOI:10.1007/BF00500016. PMID 3022160.
↑ Kitabgi P, Rostène W, Dussaillant M, Schotte A, Laduron PM, Vincent JP (August 1987). „Two populations of neurotensin binding sites in murine brain: discrimination by the antihistamine levocabastine reveals markedly different radioautographic distribution”. European Journal of Pharmacology 140 (3): 285–93. DOI:10.1016/0014-2999(87)90285-8. PMID 2888670.
↑ Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D (May 1996). „Molecular cloning of a levocabastine-sensitive neurotensin binding site”. FEBS Letters 386 (2-3): 91–4. DOI:10.1016/0014-5793(96)00397-3. PMID 8647296.
↑ Mazella J, Botto JM, Guillemare E, Coppola T, Sarret P, Vincent JP (September 1996). „Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain”. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 16 (18): 5613–20. PMID 8795617.
↑ Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A (September 2005). „Potent spinal analgesia elicited through stimulation of NTS2 neurotensin receptors”. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 25 (36): 8188–96. DOI:10.1523/JNEUROSCI.0810-05.2005. PMID 16148226.
↑ Bredeloux P, Costentin J, Dubuc I (December 2006). „Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice”. Behavioural Brain Research 175 (2): 399–407. DOI:10.1016/j.bbr.2006.09.016. PMID 17074405.
↑ Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, Nakazawa T, Yamamoto T, Wada K (September 2007). „Neurotensin type 2 receptor is involved in fear memory in mice”. Journal of Neurochemistry 102 (5): 1669–76. DOI:10.1111/j.1471-4159.2007.04805.x. PMID 17697051.

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[6] „RxMed: Pharmaceutical Information - LIVOSTIN NASAL SPRAY”. Pristupljeno 13 November 2005.

[7] Pipkorn U, Bende M, Hedner J, Hedner T., A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis. Allergy. 1985 Oct;40(7):491-6.

[pmid3022160-8] Schotte A, Leysen JE, Laduron PM (August 1986). „Evidence for a displaceable non-specific [3Hneurotensin binding site in rat brain”]. Naunyn-Schmiedeberg's Archives of Pharmacology 333 (4): 400–5. DOI:10.1007/BF00500016. PMID 3022160.

[pmid2888670-9] Kitabgi P, Rostène W, Dussaillant M, Schotte A, Laduron PM, Vincent JP (August 1987). „Two populations of neurotensin binding sites in murine brain: discrimination by the antihistamine levocabastine reveals markedly different radioautographic distribution”. European Journal of Pharmacology 140 (3): 285–93. DOI:10.1016/0014-2999(87)90285-8. PMID 2888670.

[pmid8647296-10] Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D (May 1996). „Molecular cloning of a levocabastine-sensitive neurotensin binding site”. FEBS Letters 386 (2-3): 91–4. DOI:10.1016/0014-5793(96)00397-3. PMID 8647296.

[pmid8795617-11] Mazella J, Botto JM, Guillemare E, Coppola T, Sarret P, Vincent JP (September 1996). „Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain”. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 16 (18): 5613–20. PMID 8795617.

[pmid16148226-12] Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A (September 2005). „Potent spinal analgesia elicited through stimulation of NTS2 neurotensin receptors”. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 25 (36): 8188–96. DOI:10.1523/JNEUROSCI.0810-05.2005. PMID 16148226.

[pmid17074405-13] Bredeloux P, Costentin J, Dubuc I (December 2006). „Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice”. Behavioural Brain Research 175 (2): 399–407. DOI:10.1016/j.bbr.2006.09.016. PMID 17074405.

[pmid17697051-14] Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, Nakazawa T, Yamamoto T, Wada K (September 2007). „Neurotensin type 2 receptor is involved in fear memory in mice”. Journal of Neurochemistry 102 (5): 1669–76. DOI:10.1111/j.1471-4159.2007.04805.x. PMID 17697051.

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Levokabastin

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