Mammalian olfactory receptors: pharmacology, G protein coupling and desensitization



The vertebrate olfactory system recognizes and discriminates between thousands of structurally diverse odorants. Detection of odorants in mammals is mediated by olfactory receptors (ORs), which comprise the largest superfamily of G protein-coupled receptors (GPCRs). Upon odorant binding, ORs couple to G proteins, resulting in an increase in intracellular cAMP levels and subsequent receptor signaling. In this review, we will discuss recently published studies outlining the molecular basis of odor discrimination, focusing on pharmacology, G protein activation, and desensitization of ORs. A greater understanding of the molecular mechanisms underlying OR activity may help in the discovery of agonists and antagonists of ORs, and of GPCRs with potential therapeutic applications.


Odorant Olfaction Olfactory receptor G protein Signal transduction Desensitization 



Adenylyl cyclase


β1-Adrenergic receptor


β2-Adrenergic receptor




Calcium/CaM-dependent protein kinase II

CNG channel

Cyclic nucleotide-gated channel


Guanylyl cyclase


Grueneberg ganglion


G protein-coupled receptor


GPCR kinase


Eighth intracellular helical domain


Third intracellular loop


Main olfactory epithelium


Olfactory bulb


Olfactory receptor


Olfactory sensory neuron


Polymerase chain reaction


Protein kinase A


Protein kinase C


Phospholipase C/inositol-1,4,5-triphosphate


Septal organ


Trace amine-associated receptor




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Copyright information

© Birkhäuser Verlag, Basel/Switzerland 2009

Authors and Affiliations

  1. 1.Department of Integrated BiosciencesThe University of TokyoKashiwaJapan

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