Examples of 'inverse agonist' in a sentence
Meaning of "inverse agonist"
inverse agonist: In pharmacology, an inverse agonist is a substance that binds to the same receptor as an agonist but induces a pharmacological response that is opposite to that of an agonist. It can reduce the baseline activity of a receptor and has functional effects opposite to those of agonists
How to use "inverse agonist" in a sentence
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inverse agonist
An example is the cannabinoid inverse agonist rimonabant.
Inverse agonist causes to action against to that of agonist.
This activity has been termed inverse agonist activity.
An inverse agonist is also capable of inhibiting the effect of an agonist.
The constitutive activity of a receptor may be blocked by an inverse agonist.
An inverse agonist causes an action opposite to that of the agonist.
The effect of an antagonist may also be produced by an inverse agonist.
An inverse agonist is a ligand that biases the equilibrium toward an inactive state.
Such constitutive activity might be modified vÃa contacting the relevant receptor with a synthetic inverse agonist.
The concept of an inverse agonist has been explored by Bond et al.
In some embodiments, the compound is an inverse agonist.
The method of claim 4, wherein the inverse agonist is selected from the group consisting of.
From these precursors it was possible to produce hemopressin, an inverse agonist of cb1r.
Hemopressin is an inverse agonist of CB1 cannabinoid receptors.
At high concentrations, it will diminish the actions of a full inverse agonist.
See also
The concept of a negative hormone or inverse agonist has been explored by Bond et al.
The method of claim 2 wherein the directly identified compound is an inverse agonist.
CB1 selective antagonist and inverse agonist molecules are well-known to those skilled in the art.
This locks the receptor in an inactive conformation, making the drug an inverse agonist.
The B2AR was originally crystallized bound to the inverse agonist carazolol using two different approaches.
Modulatory effect is understood in particular to mean agonist, antagonist and / or inverse agonist effects.
It is specifically a potent inverse agonist of the histamine H1 receptor.
The term is used indifferently to denote a " true " antagonist and an inverse agonist of a receptor.
It acts as an inverse agonist that decreases activity at histamine H1 receptors.
The interactions include the interactions of an agonist, partial agonist, an inverse agonist and antagonist.
GABA inverse agonist restores cognitive function in Down 's syndrome.
Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H1 receptors.
Inverse agonist of the constitutive androstane receptor ( CAR ).
Is a potent histamine H3 receptor antagonist with inverse agonist properties.
In one embodiment, the inverse agonist is the compound of formula ( I ).
Dose response curves of a full agonist, partial agonist, neutral antagonist, and inverse agonist.
The method of claim 1, wherein an inverse agonist is administered.
As used herein, " modulator " means both antagonist, partial or full agonist and inverse agonist.
Prazosin is an α1-blocker that acts as an inverse agonist at alpha-1 adrenergic receptors.
As an H1 receptor inverse agonist with high affinity, mianserin has strong antihistamine effects e.g., sedation.
It binds cannabinoid receptors, acting as an inverse agonist at CB1 receptors.
In some embodiments the inverse agonist is the compound of formula ( I ).
Pheomelanin production is controlled by the agouti-signaling protein, which is an inverse agonist of MC1R.
Hemopressin ( hp ) is an inverse agonist of cb1, which induces antinociception.
In addition, or alternatively, a modulator may act as an inverse agonist of C5a receptor.
In some embodiments the inverse agonist binds to a 5HT2A receptor or a 5HT2C receptor.
The agent may be agonist, partial agonist, antagonist or inverse agonist of CCRL2 activity.
In some embodiments the inverse agonist binds to a 5HT2A receptor and a 5HT2C receptor.
The combination of a serotonin reuptake inhibitor and a 5-HT2C antagonist, inverse agonist or partial agonist.
Preferably, the compound is an inverse agonist selective for the 5-HT2A receptor.
The human beta-2 adrenergic receptor in complex with the partial inverse agonist carazolol . [ 1 ].
Ketanserin and ritanserin have inverse agonist activity at 5-HT2A.
Preferably, the peptide is used as antagonist and / or inverse agonist of the T-type calcium channels.
The compounds of this invention preferably show selective inverse agonist activity towards the 5-HT2A receptor.
In one embodiment, the compound acts as inverse agonist at the 5-HT2A receptor.
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