Page last updated: 2024-12-11
pranidipine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
pranidipine: structure given in UD 37:228m [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 6436048 |
| SCHEMBL ID | 49274 |
| MeSH ID | M0138725 |
Synonyms (34)
| Synonym |
|---|
| acalas |
| opc-13340 |
| pranidipine |
| methyl cinnamyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 3-phenyl-2-propenyl ester, (e)- |
| trans-cinnamyl methyl 4-(3-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate |
| frc-8411 |
| pranidipine [inn] |
| ccris 6666 |
| frc 8411 |
| brn 5654325 |
| (e)-cinnamyl methyl (+-)-1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
| opc 13340 |
| 3-cinnamyl 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| 3-o-methyl 5-o-[(e)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| 99522-79-9 |
| unii-9des9qvh58 |
| 9des9qvh58 , |
| S2436 |
| pranidipine [jan] |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl (2e)-3-phenyl-2-propenyl ester |
| (e)-cinnamyl methyl (+/-)-1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate |
| 3,5-pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-methyl 5-((2e)-3-phenyl-2-propen-1-yl) ester |
| AKOS025311508 |
| SCHEMBL49274 |
| smr004701255 |
| MLS006010122 |
| HY-19664 |
| CS-0016176 |
| DTXSID00875518 |
| (z)-3-methyl 5-(3-phenylallyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| AS-15993 |
| Q7238365 |
| AKOS040742443 |
Research Excerpts
Overview
Pranidipine is an optically-active 1,4-dihydropyridine (DHP) voltage-dependent L-type calcium channel inhibitor. It is being developed for clinical use as an antihypertensive and antianginal drug.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pranidipine (OPC-13340) is a novel, potent and long-acting 1,4-dihydropyridine derivative Ca-antagonist being developed for clinical use as an antihypertensive and antianginal drug. " | ( [Effects of pranidipine (OPC-13340), a novel 1,4-dihydropyridine derivative Ca-antagonist, on isolated porcine coronary contraction and acute myocardial ischemia in the pig]. Ikezono, K; Mori, T; Nakayama, N; Ohura, M; Tominaga, M; Watanabe, K; Yabuuchi, Y, 1994) | 2.11 |
| "Pranidipine is an optically-active 1,4-dihydropyridine (DHP) voltage-dependent L-type calcium channel inhibitor. " | ( Differential properties of the optical-isomers of pranidipine, a 1,4-dihydropyridine calcium channel modulator. Fujiki, H; Hirano, T; Ikezono, K; Kido, M; Mori, T; Nakayama, N; Ohura, M; Orito, K; Sumida, T; Toide, K; Yabuuchi, Y; Yoshida, K, 1999) | 2 |
Actions
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pranidipine prevented an increase in the weight of the left and right ventricles (2.02 +/- 0.04 and 0.6 +/- 0.03g/kg, P < 0.01) and LVDd (7.9 +/-0.2mm, P < 0.01 to MI)." | ( Long-acting calcium channel antagonist pranidipine prevents ventricular remodeling after myocardial infarction in rats. Omura, T; Otsuka, R; Shimada, Y; Takeuchi, K; Ujino, K; Yoshida, K; Yoshikawa, J; Yoshiyama, M, 1999) | 1.29 |
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pranidipine treatment did not inhibit collar-induced intimal thickening." | ( The effects of calcium channel blockers are not related to their chemical structure in the collar model of the rabbit. Ertuna, E; Kerry, Z; Ozer, A; Reel, B; Yasa, M; Yetik Anacak, G, ) | 0.85 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "Oral co-administration with grapefruit juice and pranidipine was associated with increased bioavailability and changed the pharmacodynamics of pranidipine, particularly with regard to heart rate." | ( Interaction of citrus juices with pranidipine, a new 1,4-dihydropyridine calcium antagonist, in healthy subjects. Azuma, J; Hashimoto, K; Kudo, S; Matsuoka, O; Okamoto, T; Onnagawa, O; Sekino, H; Shirafuji, T, ) | 0.66 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Voltage-dependent L-type calcium channel subunit alpha-1C | Oryctolagus cuniculus (rabbit) | IC50 (µMol) | 0.0370 | 0.0370 | 0.0643 | 0.1070 | AID478862 |
| Voltage-dependent L-type calcium channel subunit alpha-1D | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0370 | 0.0013 | 1.9915 | 10.0000 | AID478861 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | IC50 (µMol) | 0.0370 | 0.0040 | 2.1555 | 7.2000 | AID478861 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Bioassays (3)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID478862 | Antagonist activity at rabbit Cav1.2 expressed in HEK293 cells assessed as inhibition of voltage pulse-induced calcium current by FLIPR calcium 4 assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
| AID478863 | Selectivity ratio of IC50 for rabbit Cav1.2 to IC50 for rat Cav1.3 | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
| AID478861 | Antagonist activity at rat Cav1.3 expressed in HEK293 cells assessed as inhibition of voltage pulse-induced calcium current by FLIPR calcium 4 assay | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Antagonism of 4-substituted 1,4-dihydropyridine-3,5-dicarboxylates toward voltage-dependent L-type Ca2+ channels Ca V 1.3 and Ca V 1.2. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (33)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (6.06) | 18.7374 |
| 1990's | 21 (63.64) | 18.2507 |
| 2000's | 9 (27.27) | 29.6817 |
| 2010's | 1 (3.03) | 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: 19.44
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 (19.44) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (8.33%) | 5.53% |
| Reviews | 2 (5.56%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 31 (86.11%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||