Compounds > declopramide
Page last updated: 2024-12-06

declopramide

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Declopramide is a potent antiemetic drug with a unique mechanism of action. It acts as a selective antagonist of the 5-HT3 receptor, a subtype of serotonin receptor found in the central and peripheral nervous systems. This receptor plays a crucial role in mediating nausea and vomiting, particularly in response to chemotherapy and radiation therapy. Declopramide's selectivity for the 5-HT3 receptor, coupled with its high affinity and rapid onset of action, makes it an effective treatment for nausea and vomiting in various clinical settings. The synthesis of declopramide involves a multi-step process starting with readily available starting materials. Declopramide is undergoing further research and clinical trials to explore its potential in other therapeutic areas, including pain management, anxiety disorders, and irritable bowel syndrome. Declopramide is studied due to its potential for improving patient quality of life and reducing the side effects of chemotherapy and other treatments.'

declopramide: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID70177
CHEMBL ID1618378
SCHEMBL ID922516
MeSH IDM0197014

Synonyms (21)

Synonym
4-amino-3-chloro-n-(2-(diethylamino)ethyl)benzamide
891-60-1
declopramide
916gjf577d ,
unii-916gjf577d
benzamide, 4-amino-3-chloro-n-(2-(diethylamino)ethyl)-
declopramide [inn]
AKOS013640677
CHEMBL1618378
SCHEMBL922516
YEYAKZXEBSVURO-UHFFFAOYSA-N
n-(2-diethylamino-ethyl)-4-amino-3-chlorobenzamide
3-chloro-procainamide
4-amino-3-chloro-n-[2-(diethylamino)ethyl]benzamide
DB06421
Q27271384
DTXSID20862460
EN300-1425545
bdbm611577
us11717500, compound declopramide
Z1222412146

Research Excerpts

Effects

ExcerptReferenceRelevance
"Declopramide has not induced central nervous system (CNS)-related side effects in rats at doses up to 200 mg/kg, whereas MCA does at 12.5 mg/kg."( Pharmacokinetics and central nervous system toxicity of declopramide (3-chloroprocainamide) in rats and mice.
Hua, J; Kane, R; Pero, RW, 1999)		1.27

Bioavailability

declopramide administered orally at 40 mg/kg gave the same efficacy of inhibiting tumor growth as im injection. oral administration had a lower bioavailability due to the formulation of N-acetyl-declopamide.

ExcerptReferenceRelevance
" In contrast to MCA, declopramide has a rapid clearance from serum, a lower tissue concentration (about 15-fold lower than MCA) and a lower oral bioavailability (about 6-fold lower than MCA)."( Pharmacokinetics and central nervous system toxicity of declopramide (3-chloroprocainamide) in rats and mice.
Hua, J; Kane, R; Pero, RW, 1999)		0.87
" declopramide administered orally at 40 mg/kg gave the same efficacy of inhibiting tumor growth as im injection although oral administration had a lower bioavailability due to the formulation of N-acetyl-declopramide."( Comparison of antitumor activity of declopramide (3-chloroprocainamide) and N-acetyl-declopramide.
Bryngelsson, C; Hua, J; Kane, R; Pero, RW; Sheng, Y, )		1.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (40.00)18.2507
2000's3 (60.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.55

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.55 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
benzamide
benzamide : An aromatic amide that consists of benzene bearing a single carboxamido substituent. The parent of the class of benzamides.		2.0110benzamides
metoclopramide
Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.		2.6930benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound		antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
acecainide
Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.. N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine.		210acetamides;
benzamides		anti-arrhythmia drug
procainamide
Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias.		8.150benzamidesanti-arrhythmia drug;
platelet aggregation inhibitor;
sodium channel blocker
igk
IgK: abnormal immunoglobin in leprous-Rubino negative sera; partly related to Fc fragment of IgA & to FAB fragments; possesses Kappa but not lambda light polypeptide chains		2.0110
ConditionIndicatedRelationship StrengthStudiesTrials
Anaplastic Astrocytoma
[description not available]		01.9910
Benign Neoplasms, Brain
[description not available]		01.9910
Astrocytoma
Neoplasms of the brain and spinal cord derived from glial cells which vary from histologically benign forms to highly anaplastic and malignant tumors. Fibrillary astrocytomas are the most common type and may be classified in order of increasing malignancy (grades I through IV). In the first two decades of life, astrocytomas tend to originate in the cerebellar hemispheres; in adults, they most frequently arise in the cerebrum and frequently undergo malignant transformation. (From Devita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2013-7; Holland et al., Cancer Medicine, 3d ed, p1082)		01.9910
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		01.9910