from Wiktionary, Creative Commons Attribution/Share-Alike License

  • adj. Describing the primary, unmodulated binding site (on a receptor) of a ligand


From ortho- +‎ steric (Wiktionary)


  • "orthosteric" drugs and the body's natural activators (i.e. endogenous ligands), glutamate in this case.

    Health News from Medical News Today

  • Under the agreement, Addex will regain rights to intellectual property and know-how and can pursue the program independently. discovers and develops an emerging class of small molecule drugs, called allosteric modulators, which have the potential to be more specific and confer significant therapeutic advantages over conventional "orthosteric" small molecule or biological drugs.

    Reuters: Press Release

  • Furthermore, Addex believes it can find specific drug-like allosteric modulators with more success than others have had with orthosteric drug discovery.

    Health News from Medical News Today

  • Although no drug specifically targeting mGluR2 is marketed, a Phase II clinical study published in Nature Medicine in 2007 showed that an orthosteric mGluR2 / 3 agonist improved symptoms of schizophrenia with efficacy similar to a leading marketed drug for schizophrenia.

    Health News from Medical News Today

  • Allosteric molecules afford modulation of receptors that is different than orthosteric drugs.

    Health News from Medical News Today

  • Separately, a related orthosteric mGluR2 / 3 agonist has been shown to have efficacy in Phase II trials in patients with generalized anxiety disorder.

    Health News from Medical News Today

  • Much like flipping a light switch on, endogenous ligands or orthosteric agonists, effectively turn receptors on, sending a message to the cell to perform a specific function.

    Health News from Medical News Today

  • This approach may prove advantageous because it allows the body to maintain control over the physiological on / off rhythm - something that no orthosteric drug has been able to emulate - while affording a new kind of therapeutic influence at disease mediating receptors.

    Health News from Medical News Today

  • Note for editors: An orthosteric agonist binds at the same site on a receptor as the endogenous ligand, in this case, glutamate.

    Health News from Medical News Today

  • The focus of the present study was to determine if M1 receptors activated by allosteric agonists undergo the same regulatory fate as M1 receptors activated by orthosteric agonists.

    BioMed Central - Latest articles


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