General Information of Drug (ID: DMUF0BJ)

Drug Name
CYTISINE Drug Info
Synonyms
CYTISINE; 485-35-8; Sophorine; Baptitoxine; (-)-Cytisine; Laburnin; Baptitoxin; Tabex; Ulexin; Cytiton; Ulexine; Tsitizin; Cytitone; Cystisine; Cytizin; Citizin; Tabax; (1R,5S)-3,4,5,6-Tetrahydro-1H-1,5-methanopyrido[1,2-a][1,5]diazocin-8(2H)-one; Baphitoxine; UNII-53S5U404NU; Cytisine (-); HSDB 3560; EINECS 207-616-0; NSC 407282; BRN 0083882; Cytisin; (1r,5s)-1,2,3,4,5,6-Hexahydro-8h-1,5-Methanopyrido[1,2-A][1,5]diazocin-8-One; CHEBI:4055; CHEMBL497939; 53S5U404NU; Cytisine, 98%
Indication
Disease Entry ICD 11 Status REF
Tobacco dependence 6C4A.2 Phase 3 [1]
Cross-matching ID
PubChem CID
10235
ChEBI ID
CHEBI:4055
CAS Number
CAS 485-35-8
TTD Drug ID
DMUF0BJ

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Neuronal acetylcholine receptor alpha-2 (CHRNA2) TTF4E0J ACHA2_HUMAN Inhibitor [2]
Neuronal acetylcholine receptor alpha-4 (CHRNA4) TT4H1MQ ACHA4_HUMAN Inhibitor [3]
Neuronal acetylcholine receptor alpha-7 (CHRNA7) TTLA931 ACHA7_HUMAN Inhibitor [4]
Neuronal acetylcholine receptor beta-2 (CHRNB2) TT5KPZR ACHB2_HUMAN Inhibitor [3]
Neuronal acetylcholine receptor beta-4 (CHRNB4) TTTVAFQ ACHB4_HUMAN Inhibitor [5]
Nicotinic acetylcholine receptor (nAChR) TTJSZTB NOUNIPROTAC Antagonist [1]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Neuronal acetylcholine receptor beta-4 (CHRNB4) DTT CHRNB4 1.678 3.621 4.217 5.389
Neuronal acetylcholine receptor beta-2 (CHRNB2) DTT CHRNB2 4.678 3.907 5.096 5.87
Neuronal acetylcholine receptor alpha-4 (CHRNA4) DTT CHRNA4 4.409 3.585 4.385 4.591
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Tobacco dependence
ICD Disease Classification 6C4A.2
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Neuronal acetylcholine receptor beta-4 (CHRNB4) DTT CHRNB4 8.30E-01 9.66E-03 0.06
Neuronal acetylcholine receptor beta-2 (CHRNB2) DTT CHRNB2 7.10E-08 -0.15 -0.85
Neuronal acetylcholine receptor alpha-4 (CHRNA4) DTT CHRNA4 3.51E-10 -0.15 -0.61
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. J Med Chem. 2006 May 4;49(9):2673-6.
3 Epibatidine isomers and analogues: structure-activity relationships. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7.
4 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97.
5 Deconstructing cytisine: The syntheses of (+/-)-cyfusine and (+/-)-cyclopropylcyfusine, fused ring analogs of cytisine. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2316-9.