The present invention describes a method for treating a disease or
condition associated with the activity of a G protein coupled receptor
(GPCR) comprising administering an inverse agonist for the GPCR, alone or
in combination with an agonist for the GPCR, to an organism with a
disease or condition associated with the activity of the GPCR in a
quantity and for a period that causes an increase in the population of
spontaneously active GPCRs associated with that physiological function,
thereby producing a therapeutic effect to ameliorate the disease or
condition. This provides a basis for so-called "paradoxical
pharmacology." These methods can be used to treat pulmonary airway
diseases, including asthma and chronic allergic rhinitis, among other
diseases and conditions, including obesity. The present invention further
describes a screening method for screening a compound for inverse agonist
activity to a GPCR.