Peringatan Keamanan

The therapeutic index of cytisine is wide.
-Large doses can interfere with breathing and cause death.
From MSDS:
orl-mus LD50:101 mg/kg ipr-mus LD50:8550 ug/kg ivn-mus LD50:1730 ug/kg scu-rat LD50:8750 ug/kg

Cytisine

DB09028

small molecule experimental

Deskripsi

Cytisine is an alkaloid naturally derived from the Fabaceae family of plants including the genera Laburnum and Cytisus. Recent studies have shown it to be a more effective and significantly more affordable smoking cessation treatment than nicotine replacement therapy. Also known as baptitoxine or sophorine, cytisine has been used as a smoking cessation treatment since 1964, and is relatively unknown in regions outside of central and Eastern Europe. Cytisine is a partial nicotinic acetylcholine agonist with a half-life of 4.8 hours. Recent Phase III clinical trials using Tabex (a brand of Cytisine marketed by Sopharma AD) have shown similar efficacy to varenicline, but at a fraction of the cost.

Struktur Molekul 2D

Berat 190.2417
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 4.8 hours.
Volume Distribusi Oral: 6.2 l/kg Oral (5 mg/kg; tested in rabbits).
Klirens (Clearance) Renal: 43 mL/min.

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Neuronal acetylcholine receptor subunit alpha-2 CHRNA2
Neuronal acetylcholine receptor subunit beta-4 CHRNB4
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Neuronal acetylcholine receptor subunit alpha-3 CHRNA3
Neuronal acetylcholine receptor subunit alpha-6 CHRNA6
Neuronal acetylcholine receptor subunit beta-2 CHRNB2

Referensi & Sumber

Synthesis reference: ORGANIC SYNTHESES, 2006, 83, 141. "Synthesis of (+)-(1R,@S,9S)-11-Methyl-7,11-Diazatricyclo7.3.1.02.7tridecane, a (+)sparteine surrogate," DOI: 10.15227/orgsyn.083.0141
Artikel (PubMed)
  • PMID: 25517706
    Walker N, Howe C, Glover M, McRobbie H, Barnes J, Nosa V, Parag V, Bassett B, Bullen C: Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62. doi: 10.1056/NEJMoa1407764.
  • PMID: 11553677
    Houlihan LM, Slater Y, Guerra DL, Peng JH, Kuo YP, Lukas RJ, Cassels BK, Bermudez I: Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors. J Neurochem. 2001 Sep;78(5):1029-43.
  • PMID: 17220536
    Tutka P, Zatonski W: Cytisine for the treatment of nicotine addiction: from a molecule to therapeutic efficacy. Pharmacol Rep. 2006 Nov-Dec;58(6):777-98.
  • PMID: 8874153
    Cooper JC, Gutbrod O, Witzemann V, Methfessel C: Pharmacology of the nicotinic acetylcholine receptor from fetal rat muscle expressed in Xenopus oocytes. Eur J Pharmacol. 1996 Aug 15;309(3):287-98.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Tabex — Sopharma AD

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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