inverse agonist

It is an inverse agonist for the cannabinoid receptor CB1.

The constitutive activity of receptors may be blocked by inverse agonist binding.

Diphenhydramine is an inverse agonist of the histamine H receptor.

It is also an inverse agonist of CB receptors.

Naloxone is an opioid inverse agonist drug developed by Sankyo in the 1960s.

It acts as an inverse agonist at melanocortin receptors, specifically, MC1.

Relative to other beta blockers, carvedilol has minimal inverse agonist activity.

This locks the receptor in an inactive conformation, making the drug an inverse agonist.

For example one 2,3-diarylpyridine derivative was shown to be potent and selective CB inverse agonist.

As well as an antagonist/inverse agonist at the following receptors:

As a high affinity H receptor inverse agonist, mianserin has strong antihistamine effects.

MRS-1706 is a selective inverse agonist for the adenosine A receptor.

Haloperidol is a dopamine inverse agonist of the typical antipsychotic class of medications.

Ciproxifan is an extremely potent histamine H inverse agonist/antagonist.

An inverse agonist can have effects similar to those of an antagonist, but causes a distinct set of downstream biological responses.

Eplivanserin is an inverse agonist on the serotonin receptor subtype 5-HT.

It is a major metabolite of hydroxyzine, and a racemic selective H receptor inverse agonist.

A-349,821 is a potent and selective histamine H receptor antagonist (or possibly an inverse agonist).

XCT790 is a potent and selective inverse agonist ligand of the estrogen-related receptor alpha.

ABT-239 is an H-receptor inverse agonist developed by Abbott.

JTE-907 is a drug used in scientific research that acts as a selective CB inverse agonist.

Valerian also contains isovaltrate, which has been shown to be an inverse agonist for adenosine A receptor sites.

A pure opioid antagonist used in medicine is naltrexone (not to be confused with naloxone, an inverse agonist).

The first specific CB receptor antagonist / inverse agonist was rimonabant, discovered in 1994.

Honokiol inhibits platelet aggregation, and works as an inverse agonist at the CB2 receptor.