National Cancer Institute Thesaurus

Last uploaded: February 23, 2024
Preferred Name

Propoxyphene

Synonyms

d-Propoxyphene

Propoxyphene

Dextropropoxyphene

4-Dimethylamino-3-methyl-1,2-diphenyl-2-propoxybutane

PROPOXYPHENE

Algafan

Antalvic

Femadol

Proxagesic

Proxyvon

SK 65

Definitions

The d-isomer of synthetic diphenyl propionate derivative propoxyphene, with narcotic analgesic effect. This agent mimics the effects of the endogenous opiate dextropropoxyphene, by binding to mu receptors located throughout the central nervous system. The binding results in GTP to GDP exchanges on the mu-G-protein complex, by which effector adenylate cyclase is inactivated thereby decreasing intracellular cAMP. This, in turn, inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, dextropropoxyphene closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels. This results in hyperpolarization, thereby reducing neuronal excitability, which further decreases the perception of pain.

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C61912

CAS_Registry

469-62-5

CHEBI_ID

CHEBI:51173

Chemical_Formula

C22H29NO2

code

C61912

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C63923

Contributing_Source

FDA

DEFINITION

The d-isomer of synthetic diphenyl propionate derivative propoxyphene, with narcotic analgesic effect. This agent mimics the effects of the endogenous opiate dextropropoxyphene, by binding to mu receptors located throughout the central nervous system. The binding results in GTP to GDP exchanges on the mu-G-protein complex, by which effector adenylate cyclase is inactivated thereby decreasing intracellular cAMP. This, in turn, inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, dextropropoxyphene closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels. This results in hyperpolarization, thereby reducing neuronal excitability, which further decreases the perception of pain.

FDA_UNII_Code

S2F83W92TK

FULL_SYN

d-Propoxyphene

Propoxyphene

Dextropropoxyphene

4-Dimethylamino-3-methyl-1,2-diphenyl-2-propoxybutane

PROPOXYPHENE

Algafan

Antalvic

Femadol

Proxagesic

Proxyvon

SK 65

Has_Salt_Form

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C29386

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C29385

label

Propoxyphene

Legacy Concept Name

Propoxyphene

Preferred_Name

Propoxyphene

prefixIRI

Thesaurus:C61912

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C0033493

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C67413

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C241

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