Preferred Name

Propoxyphene Hydrochloride

Synonyms
Definitions

The hydrochloride salt form of 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://purl.obolibrary.org/obo/NCIT_C29385

Accepted_Therapeutic_Use_For

extravasation resulting from intravenous anthracycline chemotherapy.

CAS_Registry

1639-60-7

CHEBI_ID

CHEBI:8498

Chemical_Formula

C22H29NO2.HCl

code

C29385

Contributing_Source

FDA

definition

The hydrochloride salt form of 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

CB2TL9PS0T

Has_Free_Acid_Or_Base_Form

http://purl.obolibrary.org/obo/NCIT_C61912

in_subset

http://purl.obolibrary.org/obo/NCIT_C63923

label

Propoxyphene Hydrochloride

Legacy Concept Name

Propoxyphene_Hydrochloride

NCI_Drug_Dictionary_ID

508976

NCI_META_CUI

CL449034

PDQ_Closed_Trial_Search_ID

508976

PDQ_Open_Trial_Search_ID

508976

Preferred_Name

Propoxyphene Hydrochloride

prefixIRI

NCIT:C29385

prefLabel

Propoxyphene Hydrochloride

Semantic_Type

Organic Chemical

Pharmacologic Substance

subClassOf

http://purl.obolibrary.org/obo/NCIT_C67413

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