Last update 21 Nov 2024

Propoxycaine hydrochloride

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

VGSCs

Mechanism

Voltage-gated sodium channels blockers

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure

Molecular FormulaC16H27ClN2O3

InChIKeyGITPCGSPKUQZTE-UHFFFAOYSA-N

CAS Registry550-83-4

100 Clinical Results associated with Propoxycaine hydrochloride

100 Translational Medicine associated with Propoxycaine hydrochloride

100 Patents (Medical) associated with Propoxycaine hydrochloride

Literatures (Medical) associated with Propoxycaine hydrochloride

01 Jul 2008·Chemistry and Physics of LipidsQ3 · BIOLOGY

The effect of propoxycaine·HCl on the physical properties of neuronal membranes

Q3 · BIOLOGY

Article

Author: Young Chan Jeon ; Jong Sun Park ; Hun Mun ; Jong Ho Kim ; Sung Key Lee ; Dong Il Kim ; Hye Ock Jang ; Ung Chan Yoon ; Jang Hoon Lee ; Il Yun ; Jong Hwa Lee ; W. Gibson Wood ; Moon Kyung Bae ; Yi Hoon Park

Fluorescent probe techniques were used to evaluate the effect of propoxycaine.HCl on the physical properties (transbilayer asymmetric lateral and rotational mobilities, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMVs) isolated from bovine cerebral cortex. An experimental procedure was used based on selective quenching of both 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer (RET) from the tryptophans of membrane proteins to Py-3-Py. Propoxycaine.HCl increased the bulk lateral and rotational mobilities, and annular lipid fluidity in SPMVs lipid bilayers, and had a greater fluidizing effect on the inner monolayer than that of the outer monolayer. The magnitude of increasing effect on annular lipid fluidity in SPMVs lipid bilayer induced by propoxycaine.HCl was significantly far greater than magnitude of increasing effect of the drug on the lateral and rotational mobilities of SPMVs lipid bilayer. It also caused membrane proteins to cluster. These effects of propoxycaine.HCl on neuronal membranes may be responsible for some, though not all, of the local anesthetic actions of propoxycaine.HCl.

01 Aug 2002·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

Stability-indicating HPLC assays for the determination of prilocaine and procaine drug combinations

Q3 · MEDICINE

Article

Author: Meredith L Storms ; James T Stewart

Stability-indicating, reversed phase high-performance liquid chromatographic (HPLC) methods have been developed for the determination of several procaine hydrochloride and prilocaine hydrochloride combinations. The separation and quantitation of epinephrine-prilocaine and epinephrine-procaine drug combinations were achieved on a phenyl column using a mobile phase of 80:20% v/v 25 mM phosphate buffer (pH 3.0) containing 50 mM heptanesulfonic acid sodium salt-acetonitrile at a flow rate of 1 ml x min(-1) and UV detection at 254 nm. The method showed linearity for the epinephrine and prilocaine hydrochloride mixture in the 0.25-2.5 and 8-200 micro g ml(-1) ranges, respectively. The intra- and inter-day relative standard deviations (RSDs) ranged from 0.26 to 2.05% and 0.04 to 0.61% for epinephrine and prilocaine hydrochloride, respectively. The epinephrine and procaine hydrochloride mixture yielded linear ranges of 0.25-2.0 and 5-100 micro g ml(-1) and intra- and inter-day RSDs ranged from 0.23 to 1.88% and 0.07 to 0.26% for epinephrine and procaine hydrochloride, respectively. The assays were shown to be suitable for measuring epinephrine-prilocaine and epinephrine-procaine combinations in their respective injection dosage forms. Stability-indicating HPLC assays were also developed for several other procaine drug combinations since their monographs are present in the USP 24; however, quantitation was not investigated since these combinations are not commercially available. A mobile phase consisting of 80:20% v/v 25 mM phosphate buffer (pH 3.0) containing 50 mM heptanesulfonic acid-acetonitrile was utilized for the levonordefrin-tetracaine-procaine drug combination, while a mobile phase consisting of 70:30% v/v 25 mM phosphate buffer (pH 3.0) containing 50 mM heptanesulfonic acid sodium salt-acetonitrile was utilized for the separation of levonordefrin-procaine-propoxycaine and norepinephrine-procaine-propoxycaine. All separations were achieved on a phenyl column at a flow rate of 1 ml x min(-1) and UV detection at 254 nm.

01 Apr 1995·European Journal of PharmacologyQ3 · MEDICINE

In vitro and in vivo effects of cocaine and selected local anesthetics on the dopamine transporter

Q3 · MEDICINE

Article

Author: Robert L. Balster ; David M. Compton ; Billy R. Martin ; John J. Woodward

The effects of selected local anesthetics on in vitro and in vivo measurements of dopamine transporter activity were determined to investigate the role of local anesthetic activity in the neuronal actions of cocaine. Cocaine inhibited [3H]2-beta-carbomethoxy-3-beta-(4-fluorophenyl)tropane 1.5-naphthalenedisulfonate (CFT) binding and [3H]dopamine uptake with estimated Ki and IC50 values of 0.6 microM and 0.7 micorM, respectively. Of the local anesthetics tested, only dimethocaine showed full displacement of CFT binding (0-30 microM tested) and full inhibition of dopamine uptake (0-100 microM tested). Dimethocaine was only slightly less potent than cocaine with an estimated Ki of 1.4 micorM and an IC50 value of 1.2 microM for [3H]CFT binding and dopamine uptake. At a maximum concentration of 100 microM, the ester containing local anesthetics procaine, tetracaine, piperocaine and the amide containing local anesthetic dibucaine and bupivacaine partially inhibited dopamine uptake by 47-70%. The ester containing local anesthetic propoxycaine and the amide containing local anesthetics prilocaine, etidocaine, procainamide, and lidocaine inhibited dopamine uptake by 8-30% at 100 microM. A 10 min administration of cocaine, dimethocaine, or procaine in the dialysis solution produced dose-dependent, reversible increases in endogenous dopamine efflux from the striata of awake rats. Cocaine and dimethocaine produced similar 12-fold increases in dialysate dopamine at concentrations of 0.1 mM and 1 mM respectively. Procaine (10 mM) produced a 6-fold increase in dialysate dopamine while lidocaine (1 mM) produced a reproducible and reversible decrease (30%). These results show that the cocaine-like actions of certain local anesthetics such as dimethocaine and procaine result from their direct actions of dopamine uptake inhibitors.

100 Deals associated with Propoxycaine hydrochloride

External Link

KEGG	Wiki	ATC	Drug Bank
-	Propoxycaine hydrochloride	-	DB09342

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