- |||||||||| nimodipine / Generic mfg.
Clinical, Journal: Safety of Modified Nimodipine Dosing in Aneurysmal Subarachnoid Hemorrhage. (Pubmed Central) - Aug 7, 2022
Modified dosing of nimodipine is well tolerated and may not be associated with worse functional outcome. Prospective studies are needed to better assess the relationship between nimodipine dosing and outcomes in patients with aSAH.
- |||||||||| nimodipine / Generic mfg., milrinone / Generic mfg.
Retrospective data, Journal: Nimodipine vs. Milrinone - Equal or Complementary Use? A Retrospective Analysis. (Pubmed Central) - Aug 3, 2022
Nimodipine and milrinone may be used complementary in an escalation scheme with the administration of nimodipine first, complemented by milrinone in cases of severe CVS. Milrinone monotherapy is not recommended.
- |||||||||| Tectin (tetrodotoxin) / WEX Pharma
Journal: Inactivity and Ca signaling regulate synaptic compensation in motoneurons following hibernation in American bullfrogs. (Pubmed Central) - Jul 17, 2022
Thus, inactivity drives up synaptic strength through mechanisms that do not rely on reduced L-type channel function, while Ca signaling associated with the hibernation environment independently regulates the balance of synaptic weights. Altogether, these results point to multiple feedback signals for shaping synaptic compensation that gives rise to proper network function during environmental challenges in vivo.
- |||||||||| amodiaquine hydrochloride / Generic mfg., nimodipine / Generic mfg.
Preclinical, Journal: Nurr1 Is Not an Essential Regulator of BDNF in Mouse Cortical Neurons. (Pubmed Central) - Jul 2, 2022
Membrane depolarization was induced by KCl or veratridine and reversed by nimodipine...Accordingly, the positive correlation between Nurr1 and BDNF expression in AQ and membrane depolarization experiments does not imply co-regulation because Nurr1 knockdown did not affect BDNF gene expression in resting or depolarized cortical neurons. Therefore, in contrast to midbrain dopaminergic neurons and cerebellar granule cells, Nurr1 does not regulate BDNF in cortical neurons.
- |||||||||| nimodipine / Generic mfg.
Journal: Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects. (Pubmed Central) - Jun 25, 2022
The expressions of PDE1B and PDE1C were found to be increased and concentrated in the focus of fibrosis. Compound 2g increased the levels of 3',5'-cyclic adenosine monophosphate (cAMP) and 3',5'-cyclic guanosine monophosphate (cGMP) in the lungs of rats with pulmonary fibrosis, supporting the fact that the anti-fibrosis effects of 2g were through the regulation of cAMP and cGMP.
- |||||||||| nimodipine / Generic mfg.
Journal: Ca1.2 regulated odontogenic differentiation of NG2 pericytes during pulp injury. (Pubmed Central) - Jun 25, 2022
During the odontogenic differentiation of NG2 pericytes, the effects of the Ca1.2 inhibitors, nimodipine and Ca1.2 knockdown shRNA, were analyzed by real-time polymerase chain reaction and alizarin red staining...In addition, many co-stained areas of Ca1.2 and NG2 pericytes, both near the perivascular and odontoblast layers, were observed. These results indicate that Ca1.2 played a vital role in the odontogenic differentiation of NG2 pericytes, and that it might be closely linked to the NG2 pericytes-mediated repair of dental pulp injury in vivo.
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal: Icariin attenuates ischemic stroke through suppressing inflammation mediated by endoplasmic reticulum stress signaling pathway in rats. (Pubmed Central) - Jun 22, 2022
In this study, male Sprague-Dawley rats were randomly divided into the following seven groups: sham, model, ICA low-dose (10 mg/kg), ICA medium-dose (20 mg/kg), ICA high-dose (40 mg/kg), positive control drug (12 mg/kg nimodipine) and endoplasmic reticulum stress induction (0.16 mg/kg tunicamycin) groups...(p-IRE1?), protein kinase RNA-like ER kinase (PERK), phospho-PERK (p-PERK), spliced XBP1 (XBP1s), unspliced XBP1 (XBP1u), thioredoxin-interacting protein (TXNIP), NLRP3, and caspase-1. These results suggested that ICA offers neuroprotection against ischemic stroke by inhibiting ER stress-mediated inflammation.
- |||||||||| nimodipine / Generic mfg.
Journal: Exploration on the Improvement of Cognitive Function and Inflammatory Response in Perimenopausal Patients with Mild Cognitive Impairment by Self-Prepared Ningshen Prescription. (Pubmed Central) - Jun 14, 2022
The control group was given nimodipine (Bayer Pharmaceuticals) 30 mg, 3 times/day orally, while the therapy group was given a decoction of self-prepared Ningshen prescription on the top of the control group (glossy privet fruit, mulberry, aizoon stonecrop, dan-shen root, tuber fleeceflower stem, cyperus rotundus, citron)...The differences in ALT, AST, and Cr levels between the control group and the treatment group before and after treatment were not significant (p > 0.05). Ning Shen prescription can effectively prevent the continued development of cognitive dysfunction in perimenopausal patients with MCI, delay its natural course, and can improve the patients' ability to perform daily activities and improve their TCM symptoms.
- |||||||||| nimodipine / Generic mfg.
Journal: A novel targeted nanoparticle for traumatic brain injury treatment: combined effect of ROS depletion and calcium overload inhibition. (Pubmed Central) - Jun 11, 2022
Herein, a TBI-targeted lipid covered radical scavenger nanoparticle is developed to deliver nimodipine (Np) (CL-PPS/Np), in order to inhibit Ca influx in neurons by Np and to scavenge ROS in the brain trauma microenvironment by poly(propylene sulfide) (PPS ) and thus prevent TBI-associated secondary injury...CL-PPS/Np could markedly protect the integrity of blood-brain barrier (BBB), prevent brain edema, reduce cell death and inflammatory responses, and promote functional recovery after TBI. These findings might provide a new therapy for TBI to prevent the spread of the secondary injury.
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal: Brain-Derived Extracellular Vesicles Induce Vasoconstriction and Reduce Cerebral Blood Flow in Mice. (Pubmed Central) - Jun 9, 2022
When being separated, neither protein nor phospholipid components from the lethal number of BDEVs induced vasoconstriction, reduced CBF, and caused death. These results demonstrate a novel vasoconstrictive activity of BDEVs that depends on the structure of BDEVs and contributes to TBI-induced disseminated cerebral ischemia and sudden death.
- |||||||||| cisplatin / Generic mfg., nimodipine / Generic mfg.
Journal: Nimodipine Treatment Protects Auditory Hair Cells from Cisplatin-Induced Cell Death Accompanied by Upregulation of LMO4. (Pubmed Central) - Jun 5, 2022
In addition, nimodipine pre-treatment counteracted the reduction in LIM Domain Only 4 (LMO4) by cisplatin, which was associated with increased activation of Ak strain transforming/protein kinase B (Akt), cAMP response element-binding protein (CREB), and signal transducers and activators of transcription 3 (Stat3). Thus, nimodipine presents a potentially well-tolerated substance against the ototoxicity of cisplatin, which could result in a significant improvement in patients' quality of life.
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal: TGF-β1 protects trauma-injured murine cortical neurons by upregulating L-type calcium channel Ca1.2 via the p38 pathway. (Pubmed Central) - May 26, 2022
Nimodipine, a classic LTCC blocker, abolished the protective effect of TGF-β1 on trauma-induced neuronal apoptosis...In conclusion, TGF-β1 increased trauma-injured murine cortical neuronal activity and inhibited apoptosis by upregulating Cav1.2 channels via activating the p38 MAPK pathway. Therefore, the TGF-β1/p38 MAPK/Ca 1.2 pathway has the potential to be used as a novel therapeutic target for TBI.
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal, IO biomarker: Ligustilide ameliorates cognitive impairment via AMPK/SIRT1 pathway in vascular dementia rat. (Pubmed Central) - May 22, 2022
LIG (20 or 40 mg/kg/day) and Nimodipine (20 mg/kg) were orally administered to the VaD rats for four weeks...Furthermore, LIG enhanced the expressions of P-AMPK and Sirtuin1(SIRT1) in VaD rats. In conclusion, these studies indicated that LIG could ameliorate cognitive impairment in VaD rats, which might be related to AMPK/SIRT1 pathway activation.
- |||||||||| nimodipine / Generic mfg.
Journal: Trans-Spinal Direct Current Stimulation Targets Ca Channels to Induce Persistent Motor Unit Responses. (Pubmed Central) - May 14, 2022
Administration of the L-type calcium channel blocker Nimodipine reduced spontaneous motor unit firing during c-tsDCS and blocked the persistent response...Our experimental findings, supported by computer simulation, show that c-tsDCS can target Ca conductances to augment motoneuron activity. As tsDCS is well-tolerated in humans, this knowledge informs therapeutic treatment strategies to achieve rehabilitation goals after injury; in particular, to increase muscle force.
- |||||||||| dantrolene / Generic mfg.
Preclinical, Journal: Dantrolene Significantly Improves Cerebral Blood Flow In Diabetic Rats With Cerebral Vasospasms. (Pubmed Central) - May 14, 2022
Thus, our results indicate that, in diabetic rats, 2.5 mg/kg dantrolene alone was as effective as the combination of dantrolene and the highest dose of nimodipine in reducing BFV in the MCA. Therefore, dantrolene may provide a promising alternative therapy for the treatment of CVSP in the diabetic population.
- |||||||||| nimodipine / Generic mfg., milrinone / Generic mfg.
Trial completion date, Trial initiation date, Trial primary completion date, Combination therapy: Management of Cerebral Vascular Spasm in Posttraumatic Subarachnoid Hemorrhage Using Combination Therapy (clinicaltrials.gov) - May 11, 2022
P2, N=30, Completed,
NM combined with fasudil in the treatment of aSAH induced CVS can effectively improve the VEF, alleviate IFs, and enhance the cognitive function and quality of life of patients, which is worth popularizing in clinic. Trial completion date: Jun 2021 --> Apr 2022 | Initiation date: Jul 2020 --> Aug 2021 | Trial primary completion date: Apr 2021 --> Mar 2022
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal, IO biomarker: Protective effect and mechanism of Ershiwuwei Zhenzhu Pills on cerebral apoplexy rats (Pubmed Central) - May 10, 2022
Ninety 4-weeks-old SPF male SD rats were randomly divided into 6 groups(n=15):sham operation group, model group, nimodipine group(12 mg·kg~(-1)), Ershiwuwei Zhenzhu Pills high-dose group(400 mg·kg~(-1)), Ershiwuwei Zhenzhu Pills medium-dose group(200 mg·kg~(-1)), Ershiwuwei Zhenzhu Pills low-dose group(100 mg·kg~(-1)).The permanent middle cerebral artery occlusion model(PMCAO) was established in the model group, nimodipine group, and Ershiwuwei Zhenzhu Pills groups by the improved thread plug method, while the sham operation group did not insert the thread plug.Nimodipine group and Ershiwuwei Zhenzhu Pills groups were given intragastric administration once a day for 24 days before the modeling operation, and once 1 hour before the modeling operation, while sham operation group and model group were given equal volumes of distilled water.The neuroethology of the surviving rats was measured; The volume of cerebral infarction in rats was measured by TTC method; The histopathology of rat brain was observed by HE method; The expression levels of tumor necrosis factor α(TNF-α),interleukin-1β(IL-1β),interleukin-6(IL-6),malondialdehyde(MDA),superoxide dismutase(SOD) and catalase(CAT) in serum were detected by ELISA;The mRNA expressions of Notch 1,Jagged 1,Hes 1 and Bcl-2 in rat brain were detected by RT-PCR;Western blot was used to detect the expression levels of caspase-3 protein in rat brain; the expression levels of vascular endothelial growth factor(VEGF) and CD34 positive cells in rat brain were detected by immunofluorescence.The low, medium and high dose groups of Ershiwuwei Zhenzhu Pills and nimodipine group could significantly reduce the neurobehavioral score and cerebral infarction volume of rats with permanent middle cerebral artery occlusion, reduce the morphological changes of nerve cells, decrease the expression of TNF-α,IL-1β and IL-6 in rat serum, increase the activity of SOD and CAT,and reduce the level of MDA.Furthermore, the expression levels of Notch l, Jagged l, Hes l and Bcl-2 mRNA were significantly increased, and the expression level of caspase-3 protein was decreased.Meanwhile, the number of VEGF and CD34 positive cells increased in the treatment group.The differences were statistically significant. Ershiwuwei Zhenzhu Pills has a protective effect on ischemic stroke rats, and its mechanism may be related to anti-inflammation, anti-oxidation, promotion of nerve cell proliferation, inhibition nerve cell apoptosis and promotion of angiogenesis.
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal: Nimodipine Exerts Beneficial Effects on the Rat Oligodendrocyte Cell Line OLN-93. (Pubmed Central) - Apr 22, 2022
Interestingly, the observed effects were independent of Ca1.2 and Ca1.3 because OLN-93 cells do not express these channels, and there was no measurable response pattern in patch-clamp analysis. Taking into consideration previous studies that demonstrated a beneficial effect of nimodipine on microglia, our data support the notion that nimodipine is an interesting drug candidate for the treatment of MS and other demyelinating diseases.
- |||||||||| nimodipine / Generic mfg.
Journal: Aging differentially affects LTCC function in hippocampal CA1 and piriform cortex pyramidal neurons. (Pubmed Central) - Apr 20, 2022
LTCC blocker nimodipine administration impaired spontaneous location recognition in adult rats (6-9 months)...Cav1.2 expression was similar in adult and aged PC somata, but relatively higher in PSD95- puncta in aged dendrites. Our data suggest unique features of aging-associated changes in LTCCs in the PC and hippocampus.
- |||||||||| Pivlaz (clazosentan) / Idorsia
P2 data, P3 data, Review, Journal: Lessons Learned from Phase II and Phase III Trials Investigating Therapeutic Agents for Cerebral Ischemia Associated with Aneurysmal Subarachnoid Hemorrhage. (Pubmed Central) - Apr 14, 2022
We suggest the consideration of the following strategies to improve phase II design: increased focus on the selection of surrogate markers of efficacy, selection of the optimal dose and timing of intervention, adjustment for exaggerated estimate of treatment effect in sample size calculations, use of prespecified go/no-go criteria using futility design, use of multicenter design, enrichment of the study population, use of concurrent control or placebo group, and use of innovative trial designs such as seamless phase II to III design. Modifying the design of phase II trials on the basis of lessons learned from previous phase II and phase III trial combinations is necessary to plan more effective phase III trials.
- |||||||||| nimodipine / Generic mfg.
Journal: Biocompatible poly(ethylene succinate) polyester with molecular weight dependent drug release properties. (Pubmed Central) - Apr 14, 2022
Next, this biodegradable polymer was used for the encapsulation of Ca channel blocker Nimodipine (NIMO) to overcome the poor water solubility and enhance the bioavailability of the drug...Due to the low crystallinity of PES polyester and low particle size of the encapsulated NIMO drug led to enhance solubility and releasing process of NIMO from PES with lower M (4.3 kDa and 4.5 kDa) compared to pure crystalline NIMO. However, further increasing the molecular weight (5.05 kDa) was already reduced the amount of drug release that provides the prolonged therapeutic effect and enhances the bioavailability of the NIMO drug.
- |||||||||| nimodipine / Generic mfg.
Preclinical, Journal: Updated Pharmacological Effects of Total Phenolic Acid on the Meningeal Microcirculation in Mice. (Pubmed Central) - Apr 12, 2022
The percentage of decrease was significantly decreased (P < 0.01), and the percentage of perfusion decreased in the middle and small doses of the total phenolic acid group (P < 0.05), indicating that the percentage of mice perfused decreased by the administration of each group. Total phenolic acid can reduce the percentage of mean perfusion of microcirculation in animals and reduce brain damage.
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