Drug compositions to prevent desensitization of cellular receptors

A formulation which elicits a desired response from a cellular receptor while preventing subsequent desensitization of said receptor and consisting essentially of:

• a first amount of an agonist-ligand effective for eliciting said response and suitable for ligand binding to said receptor to both high and low affinity states;
• and
• a second amount of an antagonist-ligand, mixed with from about 10−1 to about 10−6 of the first amount, effective for maximizing said response and preventing desensitization of said receptor to the agonist-ligand by binding partially in said second amount to said receptor substantially in said high affinity state to compete with the agonist-ligand for said both states.

A formulation containing an optimal ratio of an antagonist mixed with an agonist for preventing desensitization of agonist—specific cell receptors and maximizing response by said receptors comprising:

• a first amount of agonist-ligand effective for acquiring a desired response from said receptors;
• and
• a second amount of antagonist-ligand effective for inhibiting said response, said second amount in a ratio from about 10−1 to about 10−6 of said first amount of the agonist-ligand, said second amount being in proportion to the first amount as the dissociation constant of said antagonist to the square root of half the product of high affinity and low affinity dissociation constants of said agonist.