Preferred Label : Buprenorphine;
NCIt synonyms : Buprenophrine;
NCIt definition : A synthetic phenanthrene and partial agonist at the mu-opioid receptor and antagonist
at the kappa-opioid receptor, with analgesic and sedative activities, and potential
antidepressant activity and anti-hyperalgesic effect. Buprenorphine binds to and activates
the mu-opioid receptors in the central nervous system (CNS), thereby mimicking the
effects of the endogenous opiates. Binding to opioid receptors stimulates exchange
of GTP for GDP, inhibits adenylate cyclase, and decreases intracellular cAMP. This
inhibits the release of various nociceptive neurotransmitters, such as substance P,
gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin,
and somatostatin. In addition, buprenorphine closes N-type voltage-gated calcium channels
and opens calcium-dependent inwardly rectifying potassium channels, resulting in hyperpolarization,
reduced neuronal excitability, analgesia and sedation. Buprenorphine also acts as
an antagonist at the kappa-opioid receptor, which may result in antidepressant activity
and anti-hyperalgesic effect.;
UNII : 40D3SCR4GZ;
InChIKey : RMRJXGBAOAMLHD-IHFGGWKQSA-N;
CAS number : 52485-79-7;
Chemical formula : C29H41NO4;
ChEBI ID : CHEBI:3216;
Origin ID : C61656;
UMLS CUI : C0006405;
Semantic type(s)
- UMLS correspondences (same concept)
- Validated automatic mappings to BTNT
- concept_is_in_subset
- has_salt_form
- is_free_acid_or_base_form_of
