declopramide
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 Source | ID |
|---|---|
| PubMed CID | 70177 |
| CHEMBL ID | 1618378 |
| SCHEMBL ID | 922516 |
| MeSH ID | M0197014 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| "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.
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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 |
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (40.00) | 18.2507 |
| 2000's | 3 (60.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (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.
| This Compound (17.55) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 7 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||