DT-Web

DB06694 - Xylometazoline


Identification
Name Xylometazoline
Accession Number DB06694
Type small molecule
Description A nasal vasoconstricting decongestant drug which acts by binding to the same receptors as adrenaline. It is applied as a spray or as drops into the nose to ease inflammation and congestion of the nasal passageways. It binds alpha-adrenergic receptors to activate the adrenal system which causes systemic vasoconstriction, thereby easing nasal congestion.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 244.3752
Groups approved
Monoisotopic Weight 244.193948778
Pharmacology
Indication It is used for treating nasal congestion and minor inflammation due to allergies or colds.
Mechanism of action Xylometazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the result is a decrease in blood flow in the nasal passages and consequently decreased nasal congestion.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms Not Available
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Alpha-1A adrenergic receptor
Name Alpha-1A adrenergic receptor
Gene Name ADRA1A
Pharmacological action yes
Actions agonist
References
  • Yang HT, Endoh M: (+/-)-tamsulosin, an alpha 1A-adrenoceptor antagonist, inhibits the positive inotropic effect but not the accumulation of inositol phosphates in rabbit heart. Eur J Pharmacol. 1996 Oct 3;312(3):281-91. - Pubmed
  • Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. - Pubmed
DTHybrid score 0.6191
Alpha-2A adrenergic receptor
Name Alpha-2A adrenergic receptor
Gene Name ADRA2A
Pharmacological action yes
Actions agonist
References
  • Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2009 Dec 17. - Pubmed
  • Petrusewicz J, Kaliszan R: Effect of imidazoline drugs on human blood platelet aggregation. Thromb Haemost. 1985 Dec 17;54(4):784-7. - Pubmed
DTHybrid score 0.5473
Alpha-2B adrenergic receptor
Name Alpha-2B adrenergic receptor
Gene Name ADRA2B
Pharmacological action yes
Actions agonist
References
  • Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. - Pubmed
DTHybrid score 0.3531
Alpha-1B adrenergic receptor
Name Alpha-1B adrenergic receptor
Gene Name ADRA1B
Pharmacological action unknown
Actions agonist
References
  • Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. - Pubmed
DTHybrid score 0.4483
Alpha-1D adrenergic receptor
Name Alpha-1D adrenergic receptor
Gene Name ADRA1D
Pharmacological action unknown
Actions agonist
References
  • Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. - Pubmed
DTHybrid score 0.3234
Alpha-2C adrenergic receptor
Name Alpha-2C adrenergic receptor
Gene Name ADRA2C
Pharmacological action unknown
Actions agonist
References
  • Haenisch B, Walstab J, Herberhold S, Bootz F, Tschaikin M, Ramseger R, Bonisch H: Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39. - Pubmed
DTHybrid score 0.3383

Predictions


Id Partner name Gene Name Score
502 5-hydroxytryptamine 2A receptor HTR2A 0.186
23 D(1A) dopamine receptor DRD1 0.1816
831 D(2) dopamine receptor DRD2 0.1736
4512 Cytochrome P450 3A4 CYP3A4 0.1591
4119 Cytochrome P450 2D6 CYP2D6 0.1563
320 5-hydroxytryptamine 1A receptor HTR1A 0.1461
590 5-hydroxytryptamine 2C receptor HTR2C 0.1396
432 D(4) dopamine receptor DRD4 0.1215
4200 Cytochrome P450 1A2 CYP1A2 0.1192
540 Sodium-dependent noradrenaline transporter SLC6A2 0.1141
638 D(3) dopamine receptor DRD3 0.1139
163 D(1B) dopamine receptor DRD5 0.1128
725 5-hydroxytryptamine 1D receptor HTR1D 0.1113
885 5-hydroxytryptamine 1B receptor HTR1B 0.0985
492 Histamine H1 receptor HRH1 0.097
1588 Multidrug resistance protein 1 ABCB1 0.0932
766 Beta-2 adrenergic receptor ADRB2 0.0826
193 Beta-1 adrenergic receptor ADRB1 0.0785
436 5-hydroxytryptamine 2B receptor HTR2B 0.0679
716 5-hydroxytryptamine 7 receptor HTR7 0.0669
713 Sodium-dependent dopamine transporter SLC6A3 0.066
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0632
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0615
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0597
6145 Solute carrier family 22 member 1 SLC22A1 0.0597
824 Sodium-dependent serotonin transporter SLC6A4 0.0565
131 Synaptic vesicular amine transporter SLC18A2 0.055
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0549
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0537
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0536
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0529
1256 5-hydroxytryptamine 6 receptor HTR6 0.0508
6147 Solute carrier family 22 member 3 SLC22A3 0.0486
3941 Amine oxidase [flavin-containing] A MAOA 0.0475
828 Phenylalanine-4-hydroxylase PAH 0.0445
3109 Phenylalanine-4-hydroxylase phhA 0.0445
6016 Cytochrome P450 2C19 CYP2C19 0.0442
6144 Solute carrier family 22 member 2 SLC22A2 0.0438
1517 Beta-3 adrenergic receptor ADRB3 0.0424
4118 Cytochrome P450 3A5 CYP3A5 0.0418
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.04
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.04
6070 Nischarin NISCH 0.0397
4757 Cytochrome P450 2C9 CYP2C9 0.0381
709 ATP-sensitive inward rectifier potassium channel 1 KCNJ1 0.034
528 5-hydroxytryptamine 1E receptor HTR1E 0.0308
118 Organic cation/carnitine transporter 2 SLC22A5 0.0308
6013 Cytochrome P450 2E1 CYP2E1 0.0294
341 5-hydroxytryptamine 3 receptor HTR3A 0.0266
6020 Aldehyde oxidase AOX1 0.0258
6107 Cytochrome P450 3A7 CYP3A7 0.0256
587 Serum albumin ALB 0.0233
6138 Multidrug resistance protein 3 ABCB4 0.022
1636 Trace amine-associated receptor 1 TAAR1 0.0212
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0211
6030 Cytochrome P450 2B6 CYP2B6 0.0199
3939 Amine oxidase [flavin-containing] B MAOB 0.0193
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0192
465 Calmodulin CALM1 0.0186
734 D1 dopamine receptor-interacting protein calcyon CALY 0.018
124 Histamine H2 receptor HRH2 0.018
6024 Cytochrome P450 1A1 CYP1A1 0.0178
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0162
233 Potassium channel subfamily K member 2 KCNK2 0.0142
3923 Cholinesterase BCHE 0.0137
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0136
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0136
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0133
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0132
6151 Monocarboxylate transporter 10 SLC16A10 0.0129
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.0124
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0122
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.012
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.012
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0112
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.0109
4924 Cytochrome P450 2C8 CYP2C8 0.0106
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0106
833 Organic cation/carnitine transporter 1 SLC22A4 0.0096
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0095
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0093
1680 Solute carrier family 2, facilitated glucose transporter member 1 SLC2A1 0.0089
3426 Glutamine synthetase glnA 0.0084
3987 Glutamine synthetase GLUL 0.0084
3810 Catechol O-methyltransferase COMT 0.0083
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0076
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0073
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.007
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.007
4120 NADPH--cytochrome P450 reductase POR 0.0067
1656 CYP2B protein CYP2B 0.0064
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0064
3970 Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B 0.0061
401 Glutamate [NMDA] receptor subunit zeta-1 GRIN1 0.0059
164 Histamine H4 receptor HRH4 0.0058
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0056
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0054
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0054
3811 Cytochrome P450 19A1 CYP19A1 0.0052
6100 BDNF/NT-3 growth factors receptor NTRK2 0.005
696 Kappa-type opioid receptor OPRK1 0.0044
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0043
6432 Transporter snf 0.004
1618 High affinity nerve growth factor receptor NTRK1 0.0039
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0038
6859 Protein S100-A4 S100A4 0.0035
5718 Cytochrome P450 2A6 CYP2A6 0.0034
1898 Cytochrome P450 1B1 CYP1B1 0.0034
474 Acetylcholinesterase ACHE 0.0032
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.003
20 Prostaglandin G/H synthase 1 PTGS1 0.0029
3947 Xanthine dehydrogenase/oxidase XDH 0.0028
6106 Cytochrome P450 2C18 CYP2C18 0.0028
776 Bile salt export pump ABCB11 0.0026
467 Delta-type opioid receptor OPRD1 0.0024
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0024
1374 Natriuretic peptides B NPPB 0.0019
1827 Gap junction alpha-1 protein GJA1 0.0019
1908 Vascular cell adhesion protein 1 VCAM1 0.0019
194 NADH dehydrogenase [ubiquinone] 1 subunit C2 NDUFC2 0.0016
183 Vascular endothelial growth factor A VEGFA 0.0014
1360 Sphingomyelin phosphodiesterase SMPD1 0.0012
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