Norbuprenorphine
Encyclopedia
Norbuprenorphine is the primary active
metabolite
of buprenorphine
. Norbuprenorphine acts as a μ-opioid
, δ-opioid
, and nociceptin receptor
full agonist, as well as a κ-opioid receptor
partial agonist
. Norbuprenorphine crosses the blood-brain-barrier similarly to buprenorphine and likely contributes to its effects.
Biological activity
In pharmacology, biological activity or pharmacological activity describes the beneficial or adverse effects of a drug on living matter. When a drug is a complex chemical mixture, this activity is exerted by the substance's active ingredient or pharmacophore but can be modified by the other...
metabolite
Metabolite
Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...
of buprenorphine
Buprenorphine
Buprenorphine is a semi-synthetic opioid that is used...
. Norbuprenorphine acts as a μ-opioid
Mu Opioid receptor
The μ-opioid receptors are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. They are also referred to as μ opioid peptide receptors. The prototypical μ receptor agonist is the opium alkaloid morphine; μ refers to morphine...
, δ-opioid
Delta Opioid receptor
The δ-opioid receptors, also known as delta opioid receptor or simply delta receptor, abbreviated DOR, is an opioid receptor that has enkephalins as its endogenous ligands.-Function:...
, and nociceptin receptor
Nociceptin receptor
The nociceptin receptor or NOP also known as the orphanin FQ receptor or kappa-type 3 opioid receptor is a protein that in humans is encoded by the OPRL1 gene. The nociceptin receptor is a G protein-coupled receptor whose natural ligand is known as nociceptin or orphanin FQ, a 17 amino acid...
full agonist, as well as a κ-opioid receptor
Kappa Opioid receptor
The κ-opioid receptor is a protein that in humans is encoded by the OPRK1 gene. The κ-opioid receptor is one of five related receptors that bind opium-like compounds in the brain and are responsible for mediating the effects of these compounds...
partial agonist
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
. Norbuprenorphine crosses the blood-brain-barrier similarly to buprenorphine and likely contributes to its effects.