Last update 01 Nov 2024

Deserpidine

Last update 01 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(3β,16β,17α,18β,20α)-17-methoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylic acid methyl ester, 11-demethoxyreserpine, 11-desmethoxyreserpine

+ [6]

Target

VMAT2

Mechanism

VMAT2 inhibitors(Synaptic vesicular amine transporter inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

AbbVie, Inc.

Active Organization

Jilin Aodong Taonan Pharmaceutical Co., Ltd.

Inactive Organization

AbbVie, Inc.

Drug Highest PhaseApproved

First Approval Date

US (19 Apr 1957),

Hypertension

Regulation-

Structure

Molecular FormulaC32H38N2O8

InChIKeyCVBMAZKKCSYWQR-WCGOZPBSSA-N

CAS Registry131-01-1

100 Clinical Results associated with Deserpidine

100 Translational Medicine associated with Deserpidine

100 Patents (Medical) associated with Deserpidine

Literatures (Medical) associated with Deserpidine

01 Oct 2023·Journal of extracellular vesicles

Inhibition of extracellular vesicle-derived miR-146a-5p decreases progression of melanoma brain metastasis via Notch pathway dysregulation in astrocytes.

Article

Author: Nicot, Nathalie ; Thorsen, Frits ; Sundstrøm, Terje ; Utikal, Jochen ; Parajuli, Himalaya ; Nomigni, Miléne Tetsi ; Hoang, Tuyen ; Rigg, Emma ; Miletic, Hrvoje ; Lunavat, Taral R ; Wang, Jiwei ; Kreis, Stephanie ; Ystaas, Lars A R ; Xue, Zhiwei ; Li, Xingang ; Bjerkvig, Rolf ; Liu, Guowei ; Margue, Christiane ; Han, Mingzhi ; Nazarov, Petr V

Melanoma has the highest propensity of all cancers to metastasize to the brain with a large percentage of late-stage patients developing metastases in the central nervous system (CNS). It is well known that metastasis establishment, cell survival, and progression are affected by tumour-host cell interactions where changes in the host cellular compartments likely play an important role. In this context, miRNAs transferred by tumour derived extracellular vesicles (EVs) have previously been shown to create a favourable tumour microenvironment. Here, we show that miR-146a-5p is highly expressed in human melanoma brain metastasis (MBM) EVs, both in MBM cell lines as well as in biopsies, thereby modulating the brain metastatic niche. Mechanistically, miR-146a-5p was transferred to astrocytes via EV delivery and inhibited NUMB in the Notch signalling pathway. This resulted in activation of tumour-promoting cytokines (IL-6, IL-8, MCP-1 and CXCL1). Brain metastases were significantly reduced following miR-146a-5p knockdown. Corroborating these findings, miR-146a-5p inhibition led to a reduction of IL-6, IL-8, MCP-1 and CXCL1 in astrocytes. Following molecular docking analysis, deserpidine was identified as a functional miR-146a-5p inhibitor, both in vitro and in vivo. Our results highlight the pro-metastatic function of miR-146a-5p in EVs and identifies deserpidine for targeted adjuvant treatment.

01 Sep 2012·FitoterapiaQ3 · MEDICINE

Bioactivity guided isolation of antipsychotic constituents from the leaves of Rauwolfia tetraphylla L.

Q3 · MEDICINE

Article

Author: Shikha Gupta ; Anupam Maurya ; Anirban Pal ; Santosh Kumar Srivastava ; Dnyaneshwar Umrao Bawankule ; Rajendra Kumar Shukla ; Vinay Kumar Khanna

This study was undertaken to ascertain the antipsychotic properties of Rauwolfia tetraphylla L. leaves and to isolate and characterize the antipsychotic constituents. Among the MeOH extract and some alkaloidal fractions at different pHs, the alkaloidal CHCl(3) fraction at pH-9 (2C) showed the highest antipsychotic activity against dopaminergic (DA-D(2)) and serotonergic (5-HT(2A)) receptors in-vitro and amphetamine induced hyperactive mouse model in-vivo. The activity guided isolation of CHCl(3) fraction (2C) afforded six indole alkaloids: 10-methoxytetrahydroalstonine (1), isoreserpiline (2), an isomeric mixture of 11-demethoxyreserpiline (3) and 10-demethoxyreserpiline (4), α-yohimbine (5) and reserpiline (6). Given orally, alkaloids 3-6 showed significant antipsychotic activity in a dose dependent manner. None of the extract, alkaloidal fractions or alkaloids showed any extra pyramidal symptoms at the tested doses. It was also observed that MeOH extract was behaving similar to other clinically used novel atypical antipsychotics in having 5-HT(2A) occupancy greater than the DA-D(2) receptor at the tested doses. Further toxicity and safety evaluation studies of MeOH extracts of R. tetraphylla leaves at different doses (10, 100, 300 and 2000 mg/kg) on female Swiss albino mice showed that MeOH extract is non toxic. The isolated alkaloids, 3-6 could serve as a promising lead structure for drug development of treating psychotic conditions in human.

12 Apr 2011·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

Some Observations on the Pharmacology of 10-Methoxydeserpidine

Q3 · MEDICINE

Article

Author: Lewis, J J ; Mir, B J

Abstract10-Methoxydeserpidine caused a slow sustained fall in the arterial blood pressure of the anaesthetised cat when doses of 2 to 4 mg./kg. were given, an effect seen only when the initial blood pressure was high. Unlike reserpine and deserpidine, 10-methoxydeserpidine did not cause ptosis or loose stools in mice or rats when used at doses of from 10 to 80 mg./kg. and although pentobarbitone sleeping time was not increased, at higher doses of 40 to 80 mg./kg. there was reduction of motor activity, respiratory depression and some animals died. Unlike deserpidine the 10-methoxy derivative had no effect on the pressor responses to compression of the abdominal aorta or stimulation of the splanchnic nerve, but depressed the response to occlusion of the common carotid arteries. The LD50 of 10-methoxydeserpidine was found to be 82 ± 2–6 mg./kg. in mice. Methyl reserpate and reserpic acid showed reserpine-like activity in intact animals and isolated tissues only at very high doses.

100 Deals associated with Deserpidine

External Link

KEGG	Wiki	ATC	Drug Bank
D08194	Deserpidine	C02AA05	DB01089

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	CN	Jilin Aodong Taonan Pharmaceutical Co., Ltd.	16 Aug 2012

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