Drug Information

Drug (ID: DG00149) and It's Reported Resistant Information

• Name: Chlorpheniramine
• Synonyms: Allergican; Allergisan; Antagonate; Chloropheniramine; Chlorophenylpyridamin; Chlorophenylpyridamine; Chloropiril; Chloroprophenpyridamine; Chlorphenamine; Chlorphenaminum; Chlorpheniraminum; Chlorprophenpyridamine; Clofeniramina; Clorfenamina; Clorfeniramina; Cloropiril; Haynon; Hayon; Histadur; ISOCLOR; Kloromin; Phenetron; PiriIton; Piriton; Polaronil; Telachlor; Teldrin; Chlorphenamine [INN]; Clorfeniramina [Italian]; Pediacare Allergy Formula; [3H]Chlorpheniramine; Aller-Chlor; Chlo-amine; Chlor-Pro; Chlor-Trimeton Repetabs; Chlor-trimeton; Chlorphenamine (INN); Chlorphenaminum [INN-Latin]; Clofeniramina (TN); Clorfenamina [INN-Spanish]; Comakin (TN); Gen-Allerate; Novo-Pheniram; Piriton (TN); Chlor-Trimeton (TN); Chlor-Tripolon (TN); CHLORPHENIRAMINE (SEE ALSO: CHLORPHENIRAMINE MALEATE (CAS113-92-8)); Gamma-(4-Chlorophenyl)-gamma-(2-pyridyl)propyldimethylamine; Gamma-(4-Chlorophenyl)-N,N-dimethyl-2-pyridinepropanamine; 1-(p-Chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine; 1-(p-Chlorophenyl)-1-(2-pyridyl)-3-dimethylaminopropane; 2-(p-Chloro-alpha-(2-(dimethylamino)ethyl)benzyl)pyridine; 3-(4-chlorophenyl)-N,N-dimethyl-3-(pyridin-2-yl)propan-1-amine; 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine; 3-(p-Chlorophenyl)-3-(2-pyridyl)-N,N-dimethylpropylamine; 4-Chloropheniramine
• Indication:
  In total 1 Indication(s)
  Vasomotor/allergic rhinitis [ICD-11: CA08]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Validated by in-vivo Model for This Drug (1 diseases)
  Astrocytoma [ICD-11: 2F36]; [1]
• Target: Histamine H1 receptor (H1R); HRH1_HUMAN; [1]
• Formula: C16H19ClN2
• IsoSMILES: CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2
• InChI: 1S/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
• InChIKey: SOYKEARSMXGVTM-UHFFFAOYSA-N
• PubChem CID: 2725
• ChEBI ID: CHEBI:52010
• TTD Drug ID: D0B7NG
• INTEDE ID: DR0303
• DrugBank ID: DB01114

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Astrocytoma [ICD-11: 2F36]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: Chloroquine resistance transporter (CRT) [1]

• Molecule Alteration: Missense mutation; p.K76N
• Resistant Disease: Malaria [ICD-11: 1F45.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Plasmodium falciparum; 5833
• Experiment for Drug Resistance: Malaria SYBR Green I-based fluorescence (MSF) method assay
• Mechanism Description: Mutations within PfCRT, particularly changes from a charged amino acid residue (lysine, k76) to an uncharged residue (such as threonine [76T], asparagine [76N], or isoleucine [76I]), seem to be important not only in the acquisition of resistance to quinoline antimalarials (e.g., by allowing efflux of diprotic CQ), but also in the mechanism of resistance reversal actions for chemosens.

Key Molecule: Chloroquine resistance transporter (CRT) [1]

• Molecule Alteration: Missense mutation; p.K76T
• Resistant Disease: Malaria [ICD-11: 1F45.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vitro Model: Plasmodium falciparum; 5833
• Experiment for Drug Resistance: Malaria SYBR Green I-based fluorescence (MSF) method assay
• Mechanism Description: Mutations within PfCRT, particularly changes from a charged amino acid residue (lysine, k76) to an uncharged residue (such as threonine [76T], asparagine [76N], or isoleucine [76I]), seem to be important not only in the acquisition of resistance to quinoline antimalarials (e.g., by allowing efflux of diprotic CQ), but also in the mechanism of resistance reversal actions for chemosens.

References

• Ref 1: Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. doi: 10.1128/AAC.00669-07. Epub 2007 Sep 10.