RGD Reference Report - Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles. - Rat Genome Database

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Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.

Authors: Lovenberg, TW  Pyati, J  Chang, H  Wilson, SJ  Erlander, MG 
Citation: Lovenberg TW, etal., J Pharmacol Exp Ther 2000 Jun;293(3):771-8.
RGD ID: 632981
Pubmed: PMID:10869375   (View Abstract at PubMed)

The recent cloning and characterization of the human histamine H(3) receptor cDNA marked a significant step toward a greater understanding of the role of this receptor in the central nervous system. We now report the cloning of the rat histamine H(3) receptor cDNA and demonstrate distinct pharmacological species differences. The rat cDNA clone encodes a putative 445-amino acid protein with 93% identity to the human H(3) receptor. Northern blot analysis revealed a major single entity of 2.7-kb in length expressed only in brain. Transfection of the rat receptor cDNA into SK-N-MC cells conferred an ability to inhibit forskolin-stimulated cAMP formation in response to histamine and other H(3) agonists. N-[(3)H]methylhistamine saturably bound to transfected cells with high affinity (K(d) = 0.8 nM). All agonists tested had low or subnanomolar K(i) values similar to that for the human recombinant receptor. The antagonists thioperamide and clobenpropit also bound with high affinity (K(i) = 4 and 0.4 nM, respectively). This is in contrast to the antagonist profile obtained for the human recombinant receptor that showed K(i) values of 58 and 0.6 nM for thioperamide and clobenpropit, respectively. These data suggest that the low affinity of thioperamide for the human H(3) receptor represents a species difference in pharmacology and not a unique pharmacological subtype. It also was found that chloroproxyfan behaved as a full agonist at the rat recombinant receptor. These findings highlight the significance of validating the pharmacology of experimental compounds at both the rat and human H(3) receptors.



Gene-Chemical Interaction Annotations    Click to see Annotation Detail View

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
HRH3Humanclozapine multiple interactionsISOHrh3 (Rattus norvegicus)Clozapine binds to Hrh3 protein and Clozapine inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3Ratclozapine multiple interactionsEXP Clozapine binds to Hrh3 protein and Clozapine inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3Mouseclozapine multiple interactionsISOHrh3 (Rattus norvegicus)Clozapine binds to Hrh3 protein and Clozapine inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
HRH3Humanhistamine multiple interactionsISOHrh3 (Rattus norvegicus)Histamine binds to Hrh3 protein and Histamine inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3Rathistamine multiple interactionsEXP Histamine binds to Hrh3 protein and Histamine inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3Mousehistamine multiple interactionsISOHrh3 (Rattus norvegicus)Histamine binds to Hrh3 protein and Histamine inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
HRH3Humanimetit multiple interactionsISOHrh3 (Rattus norvegicus)Imetit binds to Hrh3 protein and imetit inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3Ratimetit multiple interactionsEXP Imetit binds to Hrh3 protein and imetit inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3Mouseimetit multiple interactionsISOHrh3 (Rattus norvegicus)Imetit binds to Hrh3 protein and imetit inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
HRH3HumanImmepip multiple interactionsISOHrh3 (Rattus norvegicus)Immepip binds to Hrh3 protein and Immepip inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3RatImmepip multiple interactionsEXP Immepip binds to Hrh3 protein and Immepip inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3MouseImmepip multiple interactionsISOHrh3 (Rattus norvegicus)Immepip binds to Hrh3 protein and Immepip inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
HRH3HumanN(tele)-methylhistamine affects bindingISOHrh3 (Rattus norvegicus)N(tele)-methylhistamine binds to Hrh3 proteinRGD 
Hrh3RatN(tele)-methylhistamine affects bindingEXP N(tele)-methylhistamine binds to Hrh3 proteinRGD 
Hrh3MouseN(tele)-methylhistamine affects bindingISOHrh3 (Rattus norvegicus)N(tele)-methylhistamine binds to Hrh3 proteinRGD 
HRH3HumanThioperamide multiple interactionsISOHrh3 (Rattus norvegicus)Thioperamide binds to Hrh3 protein and Thioperamide inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3RatThioperamide multiple interactionsEXP Thioperamide binds to Hrh3 protein and Thioperamide inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 
Hrh3MouseThioperamide multiple interactionsISOHrh3 (Rattus norvegicus)Thioperamide binds to Hrh3 protein and Thioperamide inhibits the reaction [N-methylhistamine binds to Hrh3 protein]RGD 

Gene Ontology Annotations    Click to see Annotation Detail View

Biological Process

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
Hrh3Ratnegative regulation of adenylate cyclase activity  IDA  RGD 

Molecular Function

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
Hrh3Ratamine binding  IPIThioperamide RGD 
Hrh3Ratheterocyclic compound binding  IPIImmepip more ... RGD 

Objects Annotated

Genes (Rattus norvegicus)
Hrh3  (histamine receptor H3)

Genes (Mus musculus)
Hrh3  (histamine receptor H3)

Genes (Homo sapiens)
HRH3  (histamine receptor H3)


Additional Information