Levokabastin 📖 Wikipedia

Levokabastin
	Atas: struktur molekular levokabastin Bawah: Representasi 3D molekul levokabastin
Data klinis
Nama dagang	Livostin
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Kategori; kehamilan	AU: B3 ; ;
Rute; pemberian	Mata, hidung
Kode ATC	R01AC02 (WHO) S01GX02;
Status hukum
Status hukum	US: ℞-only ; ℞ (Hanya resep);
Pengenal
	Nama IUPAC Asam (3S,4R)-1-[cis-4-siano-4-(4-fluorofenil)sikloheksil]-3-metil-4-fenil-4-piperidinakarboksilat;
Nomor CAS	79516-68-0 ;
PubChem CID	54385;
IUPHAR/BPS	1586;
DrugBank	DB01106 ;
ChemSpider	16736421 ;
UNII	H68BP06S81;
KEGG	D08117 ;
ChEMBL	ChEMBL1201312 ;
CompTox Dashboard (EPA)	DTXSID1048548 ;
Data sifat kimia dan fisik
Rumus	C26H29FN2O2
Massa molar	420,53 g·mol−1
Model 3D (JSmol)	Gambar interaktif;
	SMILES Fc1ccc(cc1)[C@]2(CC[C@@H](CC2)N3CC[C@@]([C@H](C)C3)(c4ccccc4)C(O)=O)C#N;
	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 ;
	(what is this?) (verify)

Levokabastin adalah antagonis reseptor H₁ generasi kedua selektif yang ditemukan oleh Janssen Pharmaceutica pada tahun 1979. Obat ini digunakan untuk konjungtivitis alergi.^[3]

Selain bertindak sebagai antihistamin, levokabastin juga kemudian ditemukan bertindak sebagai antagonis poten dan selektif untuk reseptor neurotensin NTS₂, dan merupakan obat pertama yang digunakan untuk mengkarakterisasi berbagai subtipe neurotensin.^[4]^[5] Hal ini menjadikannya alat yang berguna untuk mempelajari reseptor ini.^[6]^[7]^[8]^[9]^[10]

Obat farmasi Bilina adalah kombinasi levokabastin, benzalkonium klorida, dan komponen lainnya dan biasanya digunakan dalam suspensi 0,5 mg/ml sebagai obat tetes mata, yang dikemas dalam botol 4ml untuk pengobatan konjungtivitis alergi atau kondisi mata alergi serupa. Formulasi lain tersedia sebagai semprot hidung untuk penanganan rinitis alergi.^[11]^[12]

Referensi

sunting

^ "Livostin Nasal Spray". RxMed: Pharmaceutical Information. Diakses tanggal 13 November 2005.
^ "Livostin - levocabastine hydrochloride suspension". DailyMed. U.S. National Library of Medicine. Diakses tanggal 4 January 2016.
^ Pipkorn U, Bende M, Hedner J, Hedner T (October 1985). "A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis". Allergy. 40 (7): 491–496. doi:10.1111/j.1398-9995.1985.tb00255.x. PMID 2866725. S2CID 8681108.
^ Schotte A, Leysen JE, Laduron PM (August 1986). "Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain". Naunyn-Schmiedeberg's Archives of Pharmacology. 333 (4): 400–405. doi:10.1007/BF00500016. PMID 3022160. S2CID 23692347.
^ 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): 285–293. doi:10.1016/0014-2999(87)90285-8. PMID 2888670.
^ Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, et al. (May 1996). "Molecular cloning of a levocabastine-sensitive neurotensin binding site". FEBS Letters. 386 (2–3): 91–94. doi:10.1016/0014-5793(96)00397-3. PMID 8647296. S2CID 5802578.
^ 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. 16 (18): 5613–5620. doi:10.1523/JNEUROSCI.16-18-05613.1996. PMC 6578974. 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. 25 (36): 8188–8196. doi:10.1523/JNEUROSCI.0810-05.2005. PMC 6725526. 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. S2CID 24790151.
^ Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, et al. (September 2007). "Neurotensin type 2 receptor is involved in fear memory in mice". Journal of Neurochemistry. 102 (5): 1669–1676. doi:10.1111/j.1471-4159.2007.04805.x. PMID 17697051. S2CID 19774998.
^ "Levocabastine ophthalmic". vademecum.es. Diakses tanggal 11 September 2014.
^ "★ Levocabastina 🥇". www.vademecum.es. Diakses tanggal 2024-09-16.

Pranala luar

sunting

"Levocabastine". Drug Information Portal. U.S. National Library of Medicine. Diarsipkan dari asli tanggal June 28, 2019.
"Levocabastine hydrochloride". Drug Information Portal. U.S. National Library of Medicine. Diarsipkan dari asli tanggal January 27, 2021.

[1] "Livostin Nasal Spray". RxMed: Pharmaceutical Information. Diakses tanggal 13 November 2005.

[2] "Livostin - levocabastine hydrochloride suspension". DailyMed. U.S. National Library of Medicine. Diakses tanggal 4 January 2016.

[3] Pipkorn U, Bende M, Hedner J, Hedner T (October 1985). "A double-blind evaluation of topical levocabastine, a new specific H1 antagonist in patients with allergic conjunctivitis". Allergy. 40 (7): 491–496. doi:10.1111/j.1398-9995.1985.tb00255.x. PMID 2866725. S2CID 8681108.

[4] Schotte A, Leysen JE, Laduron PM (August 1986). "Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain". Naunyn-Schmiedeberg's Archives of Pharmacology. 333 (4): 400–405. doi:10.1007/BF00500016. PMID 3022160. S2CID 23692347.

[pmid2888670-5] 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): 285–293. doi:10.1016/0014-2999(87)90285-8. PMID 2888670.

[pmid8647296-6] Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, et al. (May 1996). "Molecular cloning of a levocabastine-sensitive neurotensin binding site". FEBS Letters. 386 (2–3): 91–94. doi:10.1016/0014-5793(96)00397-3. PMID 8647296. S2CID 5802578.

[pmid8795617-7] 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. 16 (18): 5613–5620. doi:10.1523/JNEUROSCI.16-18-05613.1996. PMC 6578974. PMID 8795617.

[pmid16148226-8] 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. 25 (36): 8188–8196. doi:10.1523/JNEUROSCI.0810-05.2005. PMC 6725526. PMID 16148226.

[pmid17074405-9] 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. S2CID 24790151.

[pmid17697051-10] Yamauchi R, Wada E, Kamichi S, Yamada D, Maeno H, Delawary M, et al. (September 2007). "Neurotensin type 2 receptor is involved in fear memory in mice". Journal of Neurochemistry. 102 (5): 1669–1676. doi:10.1111/j.1471-4159.2007.04805.x. PMID 17697051. S2CID 19774998.

[11] "Levocabastine ophthalmic". vademecum.es. Diakses tanggal 11 September 2014.

[12] "★ Levocabastina 🥇". www.vademecum.es. Diakses tanggal 2024-09-16.

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Levokabastin 📖 Wikipedia

Referensi

Pranala luar

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Data klinis

Atas: struktur molekular levokabastin Bawah: Representasi 3D molekul levokabastin
Nama dagang	Livostin
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Kategori kehamilan	AU: B3
Rute pemberian	Mata, hidung^[1]
Kode ATC	R01AC02 (WHO) S01GX02
Status hukum
Status hukum	US: ℞-only ^[2] ℞ (Hanya resep)
Pengenal
Nama IUPAC Asam (3S,4R)-1-[cis-4-siano-4-(4-fluorofenil)sikloheksil]-3-metil-4-fenil-4-piperidinakarboksilat
Nomor CAS	79516-68-0^Y
PubChem CID	54385
IUPHAR/BPS	1586
DrugBank	DB01106^Y
ChemSpider	16736421^Y
UNII	H68BP06S81
KEGG	D08117^Y
ChEMBL	ChEMBL1201312^N
CompTox Dashboard (EPA)	DTXSID1048548
Data sifat kimia dan fisik
Rumus	C₂₆H₂₉FN₂O₂
Massa molar	420,53 g·mol⁻¹
Model 3D (JSmol)	Gambar interaktif
SMILES Fc1ccc(cc1)[C@]2(CC[C@@H](CC2)N3CC[C@@]([C@H](C)C3)(c4ccccc4)C(O)=O)C#N
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^Y Key:ZCGOMHNNNFPNMX-KYTRFIICSA-N^Y
^NY (what is this?) (verify)