Drug Database
NI

nicotinic acid (nicotinic acid ER / Niaspanor / Niaspan)

✓ Approved

Merck KGaA · HCAR2 · 小分子

什么是 nicotinic acid?

nicotinic acid 是一种小分子,由Merck KGaA研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名nicotinic acid ER, Niaspanor, Niaspan
公司Merck KGaA
药物类别小分子
分子靶点HCAR2
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

nicotinic acid 作用于 1 个分子靶点:

HCAR2hydroxycarboxylic acid receptor 2 (NIACR1, GPR109A)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

nicotinic acid 针对 8 个适应症,涉及 4 个治疗领域。

治疗领域疾病/病症分期
Vascular disordersArteriosclerosis✓ Approved
Metabolism and nutrition disordersHypercholesterolaemia✓ Approved
Metabolism and nutrition disordersHypertriglyceridaemia✓ Approved
Cardiac disordersMyocardial infarction✓ Approved
Metabolism and nutrition disordersDyslipidaemia✓ Approved

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相关研究文献

PubMedNucleic acids research2026-10-27

KEGG for characterizing genomes and pathways in the biosphere.

Kanehisa Minoru M, Furumichi Miho M, Sato Yoko Y, Matsuura Yuriko Y et al.

The KEGG database (https://www.kegg.jp) has been developed as a model of the biological systems. By organizing knowledge of cellular and organism-level functions in the form of molecular wiring diagrams, the model enables generating new knowledge and finding practical applications. The KO (KEGG Orthology) dataset plays the basic role of organizing knowledge. KO is an ortholog with functional relevance, generalizing experimental evidence in specific organisms to other organisms. KEGG molecular networks, including pathway maps and modules, are generic networks with KOs as network nodes, and thus KEGG mapping from genomes to pathways can be applied to any organism. As the number of KOs increases and the KO annotation rate improves, KEGG mapping is further expanded. A set of KOs in the genome and a set of modules in the metabolic pathways are now used to characterize various data objects in the biosphere, including organisms, organism groups, microbiomes, viruses, and their combinations, such as endosymbiont-host, microbiome-host, and virus-host relationships. Furthermore, a simple measure of similarity either by KO compositions or module compositions is introduced to compare organism groups. The resulting similarity dendrograms possibly reflect similarity of cellular functions or, more specifically, metabolic functions, which can be compared with phylogenetic trees.

PMID 42934177
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PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

Changes in Adrenergic and Cholinergic Receptors on Human Cerebral Vessels.

Gatherer Maureen M, Brown Christopher C, Chinezu Laura L, Manu Doina D et al.

Background/Objectives: Sporadic cerebral amyloid angiopathy (CAA) occurs due to a failure of clearance of amyloid-beta (Aβ) along the walls of capillaries and arteries. Soluble Aβ is eliminated from the brain along the basement membranes of capillaries and arteries as Intramural Periarterial Drainage (IPAD). The motive force for IPAD is provided by the spontaneous contractions of vascular smooth muscle cells, as vasomotion. Cerebrovascular smooth muscle cells receive adrenergic and cholinergic innervation from the Locus Coeruleus and the Nucleus Basalis of Meynert, which are compromised very early in Alzheimer's disease (AD). Here, we tested the hypothesis that adrenergic and cholinergic receptors are histologically preserved in parenchymal and leptomeningeal blood vessels with CAA. Methods: Using immunohistochemistry, we examined the cerebrovascular distribution of muscarinic (M1, M2), nicotinic (α 7 nicotinic acetylcholine receptor), and adrenergic (α1b/2b) receptors in post-mortem brain tissue. We compared receptor distribution across CAA and non-CAA patients, as well as young and old patients without CAA. Results: We found significant differences in the receptor immunoreactivity of α7 nicotinic acetylcholine receptors, as well as α1b and α2b adrenergic receptors. However, there were no differences in the receptor immunoreactivity of M1 or M2 muscarinic receptors between patient groups. Conclusions: As IPAD depends on the functionality of the vascular smooth muscle cells to maintain the integrity of IPAD with aging, based on these histological findings, future therapeutic interventions could focus on agonists of α7 nicotinic acetylcholine and α1b/2b adrenergic receptors.

PMID 42943215
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PubMedEnvironmental science & technology2026-10-27

Receptor Binding Drives Toxicokinetic Processes: Insights from Two Amphipod Species Exposed to Insecticides Targeting the Nicotinic Acetylcholine Receptor.

von Au Clarissa C, Maeda Natsumi N, Raths Johannes J, Hollender Juliane J

Insecticides targeting nicotinic acetylcholine receptors (nAChRs) are used because of their high neuroactive efficacy. However, they can also exert substantial toxic pressure on nontarget aquatic invertebrates. A previous study suggested that irreversible receptor binding is the main driver of thiacloprid bioaccumulation. To determine whether the observed elimination resistance applies to other nAChR-binding insecticides and species, this study investigates five compounds from different substance classes that target nAChRs. Using the two amphipod species, Hyalella azteca and Gammarus pulex, toxicokinetic experiments were combined with assessing receptor binding in vivo and in vitro. The three N-cyanoamidines and N-nitroguanidine neonicotinoids (thiacloprid, acetamiprid, and imidacloprid) and the metabolite imidacloprid-olefin showed resistance toward elimination (i.e., over 15 days of depuration in both amphipod species). This observation could be well described by a two-compartment toxicokinetic (TK)-receptor model (>0.89 R2) with integrated irreversible binding. In contrast, the butenolide flupyradifurone was fully eliminated, and the organic biocide spinosad was eliminated significantly but slowly, both fitted well with a one-compartment TK model (>0.71 R2). These findings demonstrate that receptor-binding specificity and affinity are highly compound class dependent. Although no direct link between receptor binding and acute toxicity could be established, elimination resistance indicates a risk for delayed, sublethal effects that should be critically considered in regulatory risk assessment.

PMID 42937497
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PubMedNutrients2026-10-27

Associations of Serum Niacin and Nicotinamide with Child Behavior: A Longitudinal Study in China.

Zhang Xinhan X, Huang Kuiqing K, Liu Chen C, Wang Yi Y et al.

Background/Objectives: Nicotinic acid (NA; niacin) and nicotinamide (NAM) participate in nicotinamide adenine dinucleotide metabolism, but pediatric evidence relating serum concentrations of these vitamers to behavioral-problem scores is limited. Methods: We conducted an exploratory analysis of children assessed in Yiwu, Zhejiang Province, China, with serum NA and NAM concentrations recorded in 2021 and 2025 and caregiver-reported Child Behavior Checklist (CBCL) outcomes in 2025. Vitamin B3 was measured by high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). Internalizing, externalizing, and total-problem raw scores were the broadband outcomes; seven common raw subscales were exploratory outcomes. Multivariable linear models and three-knot restricted cubic splines (RCSs) were conducted to assess the associations between vitamin B3 and CBCL scores. Benjamini-Hochberg correction and exposure-by-sex interaction tests were used. Results: Pooled associations were compatible with the null after correction. Per interquartile-range (IQR) increase in 2021 NA, boys' adjusted contrasts were -2.18 (95% CI, -4.22 to -0.13) for internalizing, -3.04 (-5.05 to -1.04) for externalizing, and -5.33 (-9.18 to -1.47) for total problems. In sex-stratified RCS analyses, 2021 NA was associated with externalizing (q-overall = 0.040) and total problems (q-overall = 0.023) in boys, whereas 2025 NA was associated with these outcomes in girls (both q-overall = 0.042). Sex-stratified two-degree-of-freedom RCS models had limited sensitivity for small-to-modest associations. Conclusions: The sex-interaction and sex-stratified RCS patterns for NA are hypothesis-generating and require independent, prespecified replication.

PMID 42942915
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PubMedMicroorganisms2026-10-27

Shotgun Metagenomics Reveals Systemic Metabolic Pathways Promoting Organic Acid Production in Traditional Sunki Fermentation.

Oshima Asahi A, Sekiguchi Sona S, Uchikawa Shogo S, Fujita Naoya N et al.

Salt-free lacto-fermentation is gaining attention owing to the global demand for sodium reduction. Sunki, a traditional unsalted Japanese turnip pickle, provides a unique ecological model. In this study, we investigated the microbial balance and systemic metabolic pathways that promote organic acid accumulation using shotgun metagenomics. We revealed that a high-quality sunki cluster exhibiting an abundant accumulation of organic acids (lactic acid 8.58 ± 2.42 g/L, acetic acid 2.70 ± 0.76 g/L, succinic acid 1.50 ± 0.52 g/L) and low pH (3.91 ± 0.15) was characterized by the co-dominance of specific lactic acid bacteria along with the foundational species Limosilactobacillus fermentum. This co-dominance enables the synergistic operation of both the homofermentative and heterofermentative pathways, whose functional potentials positively correlated with lactic acid (r = 0.50) and acetic acid (r = 0.48) concentrations, respectively, thereby achieving both effective preservation and flavor complexity. Furthermore, we propose a dual-pathway model for succinic acid production involving the reductive tricarboxylic acid cycle from malate and the γ-aminobutyric acid (GABA) shunt. Succinic acid positively correlated with the functional potential of the GABA shunt enzyme (puuE, r = 0.57) and negatively correlated with that of glutamate dehydrogenase (gdhA, r = -0.51), suggesting a metabolic switch redirecting glutamate flux toward the GABA shunt. This mechanism highlights an advanced ecological adaptation for pH homeostasis, emphasizing that a balanced co-dominance structure determines the quality of salt-free fermented foods.

PMID 42943633
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PubMedPharmaceuticals (Basel, Switzerland)2026-10-27

The Network Pharmacology of Rosmarinic Acid and Elucidating the Wound Healing Potential of a Rosmarinic Acid-Enriched Trachystemon orientalis Extract.

Badem Merve M, Kanbolat Şeyda Ş, Ulas Çolak Nevin N, Subaş Tuğba T et al.

Background/Objectives:Trachystemon orientalis (L.) D. Don has been reported to be used in folk medicine for the treatment of inflammatory wounds and for its contained rosmarinic acid, a phenolic compound known for its antioxidant, anti-inflammatory, antimicrobial, and wound healing properties. This study aimed to obtain a rosmarinic acid-enriched extract from the aerial parts of T. orientalis and evaluate its in vitro wound healing potential. Methods: Extraction conditions were optimized using fractional factorial design and Box-Behnken optimization. Rosmarinic acid content was quantified by RP-HPLC. A rosmarinic acid-enriched extract was compared with a maceration extract and isolated rosmarinic acid. Elastase, hyaluronidase, and collagenase inhibitory activities were determined. Cytotoxicity was evaluated on L929 fibroblasts using the MTT assay, and non-cytotoxic concentrations were assessed for their effects on in vitro wound healing by scratch assay. In addition, in silico target prediction and network pharmacology analyses were performed using rosmarinic acid. Results: Optimization successfully yielded a rosmarinic acid-enriched extract from T. orientalis. The rosmarinic acid-enriched extract inhibited wound-related enzymes and enhanced wound closure in the scratch assay. Network pharmacology analysis showed putative molecular targets and signaling pathways potentially associated with the wound healing activity of rosmarinic acid, especially those involved in inflammatory responses, extracellular matrix remodeling, and tissue regeneration. Conclusions: The rosmarinic acid-enriched extract exhibited promising in vitro wound healing-related activity through the inhibition of extracellular matrix degrading enzymes and promotion of wound closure. Furthermore, network pharmacology analysis provided preliminary mechanistic insights based on computational predictions.

PMID 42943331
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