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Showing drug card for Chlorpheniramine (DB01114)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:48:16
Primary Accession Number DB01114
Secondary Accession Number
  • APRD00001
Name Chlorpheniramine
Drug Type
  • Approved
  • Small Molecule
Description A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. [PubChem]
Synonyms
  1. Chloropheniramine
  2. Chlorophenylpyridamin
  3. Chlorophenylpyridamine
  4. Chloroprophenpyridamine
  5. Chlorphenamine
  6. Chlorpheniramine Maleate
  7. Chlorprophenpyridamine
  8. Clorfeniramina
  9. Dexchlorpheniramine
  10. Dexchlorpheniramine Maleate
Brand Names
  1. Aller-Chlor
  2. Allergican
  3. Allergisan
  4. Antagonate
  5. Chlo-Amine
  6. Chlor-Trimeton
  7. Chlor-Trimeton Allergy
  8. Chlor-Trimeton Repetabs
  9. Chlor-Tripolon
  10. Chlorate
  11. Chloropiril
  12. Cloropiril
  13. Efidac 24 Chlorpheniramine Maleate
  14. Gen-Allerate
  15. Haynon
  16. Histadur
  17. Kloromin
  18. Mylaramine
  19. Novo-Pheniram
  20. Pediacare Allergy Formula
  21. Phenetron
  22. Piriton
  23. Polaramine
  24. Polaronil
  25. Pyridamal 100
  26. Telachlor
  27. Teldrin
Brand Mixtures
  1. Alka Seltzer Plus Cold Medicine Evt (Acetylsalicylic Acid + Chlorpheniramine Maleate + Phenylpropanolamine Bitartrate)
  2. Alka-Seltzer Plus Cold Medicine - Evt (Acetylsalicylic Acid + Chlorpheniramine Maleate + Phenylpropanolamine Bitartrate)
  3. Allergy Sinus Medication - Caplet (Acetaminophen + Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  4. Ana-Kit (2mg/Tab Orl, 1mg/Ml Liq Sc Im) (Chlorpheniramine Maleate + Epinephrine)
  5. Ana-Kit (Chlorpheniramine Maleate + Epinephrine Hcl)
  6. Anakit Insect Sting Treatment Kit (Chlorpheniramine Maleate + Epinephrine)
  7. Bronchodex D Cap (Chlorpheniramine Maleate + Pheniramine Maleate + Phenylpropanolamine Hydrochloride)
  8. Children's Tylenol Cold Chewable Tablets (Acetaminophen + Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  9. Children's Tylenol Cold Liquid (Acetaminophen + Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  10. Children's Tylenol Cold Liquid with Dm (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  11. Chlor Tripolon Decongest Syr (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  12. Cold Decongestant Long Acting Cap (Chlorpheniramine Maleate + Pheniramine Maleate + Phenylpropanolamine Hydrochloride)
  13. Coltalin Tablet (Acetaminophen + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  14. Contac Cold Capsules (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  15. Contac Cold Extra Strength Capsules (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  16. Contac Cough Cold and Flu Caplets (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  17. Contact C Src (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  18. Coricidin D Long Acting Tab (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  19. Coricidin D Tab (Acetylsalicylic Acid + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  20. Coricidin Sinus Headache Tab (Acetaminophen + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  21. Coricidin Tab (Acetylsalicylic Acid + Chlorpheniramine Maleate)
  22. Corsym Suspension (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  23. Counteract Sinus and Allergy (Acetaminophen + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  24. Dristan Capsules (Acetylsalicylic Acid + Caffeine + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  25. Extra Strength Allergy Plus Sinus Relief (Acetaminophen + Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  26. Extra Strength Allergy Sinus Medication (Acetaminophen + Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  27. Extra Strength Contac C - Src (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  28. Extra Strength Nighttime Cold Relief-Caplet (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  29. Extra Strength Tylenol Cold Nighttime Caplet (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  30. Extra Strength Tylenol Cold and Flu Powder (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  31. Extra Strength Tylenol Sinus Nighttime (Acetaminophen + Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  32. Grippalin & C Tab (Acetaminophen + Chlorpheniramine Maleate + Vitamin C)
  33. Neocitran Total (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  34. Omni-Tuss Sus (Chlorpheniramine + Codeine + Ephedrine As Resin Complex + Guaiacol Carbonate + Phenyltoloxamine)
  35. Once-a-Day Benylin Cold Cap (Chlorpheniramine Maleate + Pseudoephedrine Hydrochloride)
  36. Ornade Af Liquid (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  37. Ornade Af Spansule Src (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  38. Ornade Dm 10 Liq (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  39. Ornade Dm 15 Liq (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  40. Ornade Dm 30 Liq (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Phenylpropanolamine Hydrochloride)
  41. Ornade Expectorant Cough Formula (Chlorpheniramine Maleate + Guaifenesin + Phenylpropanolamine Hydrochloride)
  42. Ornade Liquid (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  43. Ornade Spansule Src (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  44. Pendamine (Chlorpheniramine Maleate + Dexamethasone + Dihydrostreptomycin Sulfate + Penicillin G Procaine)
  45. Pentuss Srs (Chlorpheniramine Maleate + Codeine)
  46. Reg.Str.Cold Medic. (Night Time Relief)Caplet (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  47. Regular Strength Tylenol Cold Nighttime Caplet (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  48. Regular Strength Tylenol Cold and Flu Powder (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  49. Rhinofebral (Chlorpheniramine Maleate + Acetaminophen + Vitamin C)
  50. Sine-Off Allergy Tab (Acetaminophen + Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  51. Theraflu Flu Cold and Cough Medicine (Acetaminophen + Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
  52. Tri-Anamine Cold Syrup (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  53. Triaminic Cold and Allergy Syrup (Chlorpheniramine Maleate + Phenylpropanolamine Hydrochloride)
  54. Triaminic Dm Expectorant Syr (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Guaifenesin + Pseudoephedrine Hydrochloride)
  55. Triaminic Expectorant Syr (Chlorpheniramine Maleate + Guaifenesin + Pseudoephedrine Hydrochloride)
  56. Triaminicol Dm Syrup (Chlorpheniramine Maleate + Dextromethorphan Hydrobromide + Pseudoephedrine Hydrochloride)
Chemical IUPAC Name 3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Chemical Formula C16H19ClN2
Chemical Structure Structure
CAS Registry Number 132-22-9
InChI Identifier InChI=1/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
InChI Key SOYKEARSMXGVTM-UHFFFAOYAD
KEGG Drug D07398 Link Image
KEGG Compound C06905 Link Image
PubChem Compound 2725 Link Image
PubChem Substance 151743 Link Image
ChEBI ID Not Available
PharmGKB ID PA448960 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02265559 Link Image
RxList Link http://www.rxlist.com/cgi/generic/chlorpheniramine.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Chlorpheniramine Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 274.7880
Monoisotopic Molecular Weight 274.1237
State Liquid
Melting Point 142 oC (boiling point)
Experimental Water Solubility 5.5 g/L Source: PhysProp
Predicted Water Solubility 5.19e-02 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 3.2 Source: PhysProp
Predicted LogP 3.74 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -3.72 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 9.13
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES CN(C)CC[C@H](C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Canonical SMILES CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Drug Category
  • Anti-Allergic Agents
  • Antihistamines
  • Antipruritics
  • Histamine H1 Antagonists
ATC Codes
AHFS Codes
  • 04:04.20
Indication For the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever.
Pharmacology In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis, vasodilatation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability and potentiates pain. Chlorpheniramine, is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies.
Mechanism of Action Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
Absorption Well absorbed in the gastrointestinal tract.
Toxicity LD50 = 306 mg/kg in humans, mild reproductive toxin to women of childbearing age.
Protein Binding 72%
Biotransformation Primarily hepatic via Cytochrome P450 (CYP450) enzymes.
Half Life 21-27 hours
Dosage Forms
Form Route
Syrup Oral
Tablet Oral
Tablet, extended release Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Donepezil Possible antagonism of action
Ethotoin The antihistamine increases the effect of hydantoin
Fosphenytoin The antihistamine increases the effect of hydantoin
Galantamine Possible antagonism of action
Mephenytoin The antihistamine increases the effect of hydantoin
Phenytoin The antihistamine increases the effect of hydantoin
Rivastigmine Possible antagonism of action
Food Interactions
  • Avoid alcohol.
  • Take with food.
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A4 (CYP3A4)
  2. Cytochrome P450 2D6 (CYP2D6)
Targets
  1. Histamine H1 receptor
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 1 Gene Name CYP3A4
Enzyme 1 SwissProt ID P08684 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 2D6 (CYP2D6)
Enzyme 2 Gene Name CYP2D6
Enzyme 2 SwissProt ID P10635 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P10635|CP2D6_HUMAN Cytochrome P450 2D6 (EC 1.14.14.1) 
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQ
LRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVF
LARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDK
AVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKV
LRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVA
DLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVI
HEVQRFGDIVPLGMTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHF
LDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGV
FAFLVSPSPYELCAVPR
Drug Target 1 [top]
Target 1 ID 492
Target 1 Name Histamine H1 receptor
Target 1 Synonyms Not Available
Target 1 Gene Name HRH1
Target 1 Protein Sequence >Histamine H1 receptor 
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
Target 1 Number of Residues 495
Target 1 Molecular Weight 55785
Target 1 Theoretical pI 9.58
Target 1 GO Classification
Function
amine receptor activity
histamine receptor activity
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 30-49
  • 64-83
  • 102-123
  • 146-165
  • 190-210
  • 419-438
  • 451-470
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 510296 Link Image
Target 1 UniProtKB/Swiss-Prot ID P35367 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name HRH1_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1464 bp 
ATGAGCCTCCCCAATTCCTCCTGCCTCTTAGAAGACAAGATGTGTGAGGGCAACAAGACC
ACTATGGCCAGCCCCCAGCTGATGCCCCTGGTGGTGGTCCTGAGCACTATCTGCTTGGTC
ACAGTAGGGCTCAACCTGCTGGTGCTGTATGCCGTACGGAGTGAGCGGAAGCTCCACACT
GTGGGGAACCTGTACATCGTCAGCCTCTCGGTGGCGGACTTGATCGTGGGTGCCGTCGTC
ATGCCTATGAACATCCTCTACCTGCTCATGTCCAAGTGGTCACTGGGCCGTCCTCTCTGC
CTCTTTTGGCTTTCCATGGACTATGTGGCCAGCACAGCGTCCATTTTCAGTGTCTTCATC
CTGTGCATTGATCGCTACCGCTCTGTCCAGCAGCCCCTCAGGTACCTTAAGTATCGTACC
AAGACCCGAGCCTCGGCCACCATTCTGGGGGCCTGGTTTCTCTCTTTTCTGTGGGTTATT
CCCATTCTAGGCTGGAATCACTTCATGCAGCAGACCTCGGTGCGCCGAGAGGACAAGTGT
GAGACAGACTTCTATGATGTCACCTGGTTCAAGGTCATGACTGCCATCATCAACTTCTAC
CTGCCCACCTTGCTCATGCTCTGGTTCTATGCCAAGATCTACAAGGCCGTACGACAACAC
TGCCAGCACCGGGAGCTCATCAATAGGTCCCTCCCTTCCTTCTCAGAAATTAAGCTGAGG
CCAGAGAACCCCAAGGGGGATGCCAAGAAACCAGGGAAGGAGTCTCCCTGGGAGGTTCTG
AAAAGGAAGCCAAAAGATGCTGGTGGTGGATCTGTCTTGAAGTCACCATCCCAAACCCCC
AAGGAGATGAAATCCCCAGTTGTCTTCAGCCAAGAGGATGATAGAGAAGTAGACAAACTC
TACTGCTTTCCACTTGATATTGTGCACATGCAGGCTGCGGCAGAGGGGAGTAGCAGGGAC
TATGTAGCCGTCAACCGGAGCCATGGCCAGCTCAAGACAGATGAGCAGGGCCTGAACACA
CATGGGGCCAGCGAGATATCAGAGGATCAGATGTTAGGTGATAGCCAATCCTTCTCTCGA
ACGGACTCAGATACCACCACAGAGACAGCACCAGGCAAAGGCAAATTGAGGAGTGGGTCT
AACACAGGCCTGGATTACATCAAGTTTACTTGGAAGAGGCTCCGCTCGCATTCAAGACAG
TATGTATCTGGGTTGCACATGAACCGCGAAAGGAAGGCCGCCAAACAGTTGGGTTTTATC
ATGGCAGCCTTCATCCTCTGCTGGATCCCTTATTTCATCTTCTTCATGGTCATTGCCTTC
TGCAAGAACTGTTGCAATGAACATTTGCACATGTTCACCATCTGGCTGGGCTACATCAAC
TCCACACTGAACCCCCTCATCTACCCCTTGTGCAATGAGAACTTCAAGAAGACATTCAAG
AGAATTCTGCATATTCGCTCCTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID HRH1 Link Image
Target 1 GenAtlas ID HRH1 Link Image
Target 1 HGNC ID HGNC:5182 Link Image
Target 1 Chromosome Location 3
Target 1 Locus 3p25
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Fukui H, Fujimoto K, Mizuguchi H, Sakamoto K, Horio Y, Takai S, Yamada K, Ito S: Molecular cloning of the human histamine H1 receptor gene. Biochem Biophys Res Commun. 1994 Jun 15;201(2):894-901. [PubMed Link Image]
  2. De Backer MD, Gommeren W, Moereels H, Nobels G, Van Gompel P, Leysen JE, Luyten WH: Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. Biochem Biophys Res Commun. 1993 Dec 30;197(3):1601-8. [PubMed Link Image]
Target 1 Drug References
  1. Hasenohrl RU, Kuhlen A, Frisch C, Galosi R, Brandao ML, Huston JP: Comparison of intra-accumbens injection of histamine with histamine H1-receptor antagonist chlorpheniramine in effects on reinforcement and memory parameters. Behav Brain Res. 2001 Oct 15;124(2):203-11. [PubMed Link Image]
  2. Tagawa M, Kano M, Okamura N, Higuchi M, Matsuda M, Mizuki Y, Arai H, Iwata R, Fujii T, Komemushi S, Ido T, Itoh M, Sasaki H, Watanabe T, Yanai K: Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol. 2001 Nov;52(5):501-9. [PubMed Link Image]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  4. Nicholson AN, Pascoe PA, Turner C, Ganellin CR, Greengrass PM, Casy AF, Mercer AD: Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene. Br J Pharmacol. 1991 Sep;104(1):270-6. [PubMed Link Image]
  5. Yasuda SU, Wellstein A, Likhari P, Barbey JT, Woosley RL: Chlorpheniramine plasma concentration and histamine H1-receptor occupancy. Clin Pharmacol Ther. 1995 Aug;58(2):210-20. [PubMed Link Image]
  6. Salata JJ, Jurkiewicz NK, Wallace AA, Stupienski RF 3rd, Guinosso PJ Jr, Lynch JJ Jr: Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ Res. 1995 Jan;76(1):110-9. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.