Structure of Nifedipine
CAS No.: 21829-25-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Nifedipine is a calcium channel blocker with high affinity for L-type calcium channels, with an IC50 value of 10 nM. Nifedipine has antihypertensive and antianginal effects and can be used in cardiovascular disease research.
Synonyms: BAY-a-1040; BAY 1040
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Fofie, Christian Kuete ; Granja-Vazquez, Rafael ; Truong, Vincent ; Walsh, Patrick ; Price, Theodore ; Biswas, Swati , et al.
Abstract: Chronic pain is a global health issue, yet effective treatments remain limited due to poor preclinical-to-human translation. To address this, we developed a high-content screening (HCS) platform using hiPSC-derived nociceptors to identify analgesics targeting the peripheral nervous system. These cells, cultured on multi-well microelectrode arrays, achieved nearly 100% active electrodes by week 2, maintaining stable activity for at least 2 weeks. After 28 days, we assessed drug effects on neuronal activity, achieving strong assay performance (robust Z′ > 0.5). Pharmacological tests confirmed responses to key analgesic targets, including ion channels (Nav, Cav, Kv, and TRPV1), neurotransmitter receptors (AMPAR and GABA-R), and kinase inhibitors (tyrosine and JAK1/2). Transcriptomic analysis validated target expression, though levels differed from primary human DRG cells. The platform was used to screen over 700 natural compounds, demonstrating its potential for analgesic discovery. This HCS platform facilitates the rapid discovery of uncharacterized analgesics, reducing preclinical-to-human translation failure.
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CAS No. : | 21829-25-4 |
Formula : | C17H18N2O6 |
M.W : | 346.33 |
SMILES Code : | O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC |
Synonyms : |
BAY-a-1040; BAY 1040
|
MDL No. : | MFCD00057326 |
InChI Key : | HYIMSNHJOBLJNT-UHFFFAOYSA-N |
Pubchem ID : | 4485 |
GHS Pictogram: |
![]() ![]() |
Signal Word: | Warning |
Hazard Statements: | H302-H351-H361 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Gastric fundus smooth muscle cells | 10 µM | Nifedipine was used to block L-type calcium currents to study the electrophysiological properties of gastric fundus smooth muscle cells | Int J Mol Sci. 2023 Jan 5;24(2):1082. | |
HVC X neurons | 10 μM | Used to block L-type calcium channels to study their effect on neuronal activity. | Nat Commun. 2020 Feb 19;11(1):952. | |
Rat aortic smooth muscle cells | 25 nM and 100 nM | 30 min | To investigate the effect of Nifedipine on Ang II-induced NADPH oxidase activity, results showed that Nifedipine significantly attenuated Ang II-induced NADPH oxidase activity. | J Mol Cell Cardiol. 2015 Oct;87:152-9. |
Human myometrial smooth muscle cells (PHM1-41) | 10 µM | 48 h | To assess the effect of nifedipine on the contractility of myometrial smooth muscle cells. Results showed that nifedipine inhibited TNF/LPS-induced contraction, maintaining a level of contraction similar to the basal vehicle control conditions at 48 h. | Sci Rep. 2023 Apr 6;13(1):5646. |
Human myometrial smooth muscle cells (PHM1-41) | 10 µM | 24 h | To assess the effect of nifedipine on the inflammatory response of myometrial smooth muscle cells. Results showed that nifedipine did not reduce TNF or LPS-induced pro-inflammatory cytokine gene expression. | Sci Rep. 2023 Apr 6;13(1):5646. |
CAFs | 2.5 μM | 24 h | To evaluate the effect of Nifedipine on CAF activated phenotype, results showed that Nifedipine reduced CAF motility and ECM remodeling ability | J Exp Clin Cancer Res. 2024 Jun 11;43(1):161. |
WPMY-1 | 2.5 μM | To evaluate the effect of Nifedipine on inward current in WPMY-1 cells, results showed that Nifedipine significantly reduced the inward current | J Exp Clin Cancer Res. 2024 Jun 11;43(1):161. | |
Gastric smooth muscle cells | 10 μM | 1-2 min | Nifedipine was used to block L-type Ca2+ channels to study the effect of ADPN on Ca2+ currents in gastric smooth muscle cells. The results showed that ADPN reduced the amplitude of Ca2+ currents. | Int J Mol Sci. 2020 Dec 17;21(24):9617. |
LNCaP | 70 μM | 24 h | To study the effects of Nifedipine on prostate cancer cells, the results showed that 635 proteins (12.61%) showed significant differences between the treatment and control groups, including 89 upregulated proteins and 147 downregulated proteins. | Cancer Biol Med. 2021 Apr 24;19(1):74–89. |
DU145 | 26.66 ± 19.26 μM | 72 h | To study the effects of Nifedipine on prostate cancer cells, the results showed that Nifedipine produced dose-dependent antiproliferative effects in DU145 cells. | Cancer Biol Med. 2021 Apr 24;19(1):74–89. |
MGC-803 | 20.73 ± 10.10 μM | 72 h | To study the effects of Nifedipine on gastric cancer cells, the results showed that Nifedipine showed toxicity in the MGC-803 cell line. | Cancer Biol Med. 2021 Apr 24;19(1):74–89. |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
C57BL/6 mice | SFTSV infection model | Intragastric administration | 100 mg/kg | Twice a day for 7 days | Benidipine hydrochloride and nifedipine significantly reduced viral loads in spleen and serum, and alleviated SFTSV-induced pathogenesis. | Cell Res. 2019 Sep;29(9):739-753. |
Mice | FVB/N mice | Apical administration | 10 µmol/L | Single dose | To evaluate the effect of nifedipine on Ca2+ absorption in the ileum of P14 mice, results showed that nifedipine significantly inhibited Ca2+ absorption. | Cell Mol Gastroenterol Hepatol. 2019;8(4):625-642 |
Mice | Awake and freely moving CD-1 male mice | Intraperitoneal injection | 1 mg/kg | Single administration, observed for 5 hours | Nifedipine (1 mg/kg) did not significantly alter the basal HR in vehicle-treated mice, and it did not modify the effect provoked by JWH-018 injection. The JWH-018-induced tachyarrhythmias were slightly reduced after nifedipine injection in the last two hours of experiment. Nifedipine slightly reduced basal BR one hour following the treatment, and in JWH-018-pretreated mice, it abolished the reduction of breath rate during the first hour of the experiment. The effect on oxygen saturation subsequent to nifedipine administration did not reveal a difference from the vehicle. However, nifedipine was able to slightly increase oxygen saturation immediately after injection when it was administered after JWH-018. | Int J Mol Sci. 2023 Apr 19;24(8):7515 |
Hph-1 mice | Ang II-induced abdominal aortic aneurysm model | Oral | 5 mg/kg and 20 mg/kg | Once daily for 14 days | To investigate the effect of Nifedipine on the formation of abdominal aortic aneurysm, results showed that Nifedipine significantly reduced the incidence of AAA and improved eNOS coupling state and NO bioavailability. | J Mol Cell Cardiol. 2015 Oct;87:152-9. |
Mice | LPS-induced preterm birth model | Intraperitoneal injection | 1 mg/kg or 10 mg/kg | Every 24 hours until birth | To assess the effect of nifedipine on preventing LPS-induced preterm birth. Results showed that nifedipine was unable to consistently delay preterm birth, although it prolonged pregnancy in some mice. | Sci Rep. 2023 Apr 6;13(1):5646. |
SCID mice | Prostate cancer xenograft model | Intratumoral injection | 250 μl | 5 consecutive days for 2 weeks | To evaluate the effect of Nifedipine-treated CAF conditioned medium on prostate cancer xenograft growth, results showed that Nifedipine significantly attenuated tumor growth | J Exp Clin Cancer Res. 2024 Jun 11;43(1):161. |
Male nude mice | Prostate cancer xenograft model | Intraperitoneal injection | 50 mg/kg | Daily for 15 days | To study the effects of Nifedipine on prostate tumor growth, the results showed that Nifedipine significantly inhibited the growth and proliferation of tumors. | Cancer Biol Med. 2021 Apr 24;19(1):74–89. |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT00137501 | Labor, Premature | PHASE3 | TERMINATED | 2025-06-09 | American University of Beirut ... More >>Medical Center, Beirut, Lebanon Less << |
NCT00185952 | Obstetric Labor, Premature|Ven... More >>ous Thrombosis Less << | COMPLETED | 2025-08-08 | Stanford University School of ... More >>Medicine, Stanford, California, 94305, United States Less << | |
NCT02072291 | Embryo Implantation | PHASE2 | UNKNOWN | 2025-06-18 | Hadassah Medical Organization,... More >> Jerusalem, Israel Less << |
NCT01351428 | Pre-Eclampsia|Pregnancy|Hypert... More >>ension Less << | COMPLETED | 2025-11-12 | Mount Sinai Hospital, Toronto,... More >> Ontario, M5G1X5, Canada Less << | |
NCT00000102 | Congenital Adrenal Hyperplasia | PHASE1|PHASE2 | COMPLETED | - | Medical University of South Ca... More >>rolina, Charleston, South Carolina, United States Less << |
NCT02527109 | Chronic Anal Fissure | PHASE2|PHASE3 | COMPLETED | 2018-08-22 | UMHAT "Sveti Georgi", Internal... More >> Consulting Department, Plovdiv, Bulgaria|"Multiprofile Hospital for Active Treatment - Doverie" AD, Clinic of Gastroenterology, Sofia, 1632, Bulgaria|II MHAT, Internal Clinic, Department of Gastroenterology, Sofia, Bulgaria|MC Health BG EOOD, Sofia, Bulgaria|Multiprofile Hospital for Active Treatment Lulin, Sofia, Bulgaria|MC "New rehabilitation centre'' EOOD, Stara Zagora, Bulgaria|"Multiprofile Regional Hospital for Active Treatment - Dr. St. Cherkezov" AD Department of Gastroenterology, Veliko Tarnovo, 5002, Bulgaria|IMSP Spitalul Clinic Municipal Nr 1, Chisinau, Moldova, Republic of|IMSP Spitalul Clinic Municipal Nr 3 "Sfanta Treime", Chisinau, Moldova, Republic of|IMSP Spitalul Clinic Republican, Chisinau, Moldova, Republic of|Med-Gastr Centrum Medyczne, Lodz, 91-034, Poland|Ambulatorium Medyczne Medical Hair & Esthetic, Lublin, 20-844, Poland|Centrum Innowacyjnych Terapii Sp. z o.o. Oddzia? w Piasecznie, Piaseczno, 05-500, Poland|NZOZ Specjalistyczne Centrum Medyczne Flebo, Wolomin, 05-200, Poland|Pelican Impex SRL, Oradea, Jud. Bihor, 410469, Romania|IRGH, Cluj Napoca, Jud. Cluj, 400162, Romania|Tvm Med Serv Srl, Cluj Napoca, Jud. Cluj, Romania|Institutul Regional de Gastroenterologie si Hepatologie "Prof. Dr. Octavian Fodor", Cluj-Napoca, Jud. Cluj, 400162, Romania|SC Schnelbach Medical Care SRL, Ploiesti, Jud. Prahova, Romania|Spit. Clinic Judetean de Urgenta "Sf. Apostol Andrei" Constanta, Constanta, Judet Constanta, Romania|Dacmed SRL, Ploiesti, Judetul Prahova, Romania|Centrul Medical de Diagnostic si Tratament Ambulator Neomed SRL, Brasov, 500283, Romania|Institutul Clinic Fundeni, Bucharest, 022328, Romania|Centrul Medical Sfanta Vineri SRL, Bucharest, Romania Less << |
NCT02090920 | Preterm Labor | COMPLETED | 2025-04-19 | Eskenazi Health, Indianapolis,... More >> Indiana, 46202, United States|IU Health Methodist, Indianapolis, Indiana, 46202, United States Less << | |
NCT00244530 | Kidney Failure, Chronic|Corona... More >>ry Artery Disease Less << | PHASE4 | COMPLETED | 2025-10-05 | Rikshospitalet University Hosp... More >>ital, Oslo, 0027, Norway Less << |
NCT02068404 | Preterm Labor | PHASE4 | UNKNOWN | 2025-01-16 | Centre Hospitalier Universitai... More >>re Vaudois, Lausanne, Vaud, 1011, Switzerland Less << |
Tags: Nifedipine | BAY-a-1040 | Calcium Channel | Autophagy | Ca2+ channels | Ca channels | Calcium Channel Blocker | Ca2+ channel | Ca channel | dihydropyridine | L-type calcium channels | hypertension treatment | angina management | 21829-25-4
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