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cocaine hydrochloride (Numbrino)

✓ Approved

Lannett · SCN5A · 小分子

什么是 cocaine hydrochloride？

cocaine hydrochloride 是一种小分子，由Lannett研发。该药已获批，用于治疗相关适应症，给药途径：Topical。

药物档案

商品名Numbrino
公司Lannett
药物类别小分子
分子靶点SCN5A
给药途径Topical
状态Approved
来源： ClinicalTrials.gov, Lannett

作用机制

分子靶点

cocaine hydrochloride 作用于 1 个分子靶点：

SCN5Asodium voltage-gated channel alpha subunit 5 (CMD1E, SSS1)
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

cocaine hydrochloride 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersAnaesthesia✓ Approved
Nervous system disordersSensory loss✓ Approved

相关研究文献

PubMedPsychopharmacology2026-10-26

Evaluating whether a therapeutic dose of ketamine exposure during adolescence influences adult vulnerability in rats to commonly abused drugs.

Jornet-Plaza Jordi J, Colom-Rocha Carles C, García-Fuster M Julia MJ

Rationale Ketamine has emerged as a rapid-acting antidepressant drug for treatment-resistant depression in adults and is currently evaluated for adolescent depression. However, the long-term effects of ketamine exposure during this period of brain development remain unclear, particularly regarding addiction liability. Objectives To investigate whether repeated ketamine exposure during adolescence may influence the long-term risk of addiction following subsequent exposure to commonly abused drugs (alcohol and cocaine) in adulthood. Methods Male and female Sprague-Dawley rats received daily i.p. injections of ketamine (10 mg/kg) or saline for 7 consecutive days during mid adolescence. The dose paradigm of ketamine administered was selected based on its antidepressant-like properties in adolescent rats. In adulthood, addiction liability was measured by voluntary ethanol consumption, using a two-bottle choice paradigm, and by assessing cocaine reward using a single-exposure place preference protocol. Results The main results suggested that a therapeutic dose of ketamine exposure during adolescence did not enhance addictive liability in adulthood as measured by voluntary ethanol consumption or cocaine reward in rats of both sexes. Conclusions Ketamine, administered during adolescence at a dose known to induce antidepressant-like effects did not impact the long-term risk of addiction caused by exposure to commonly abused drugs (i.e., alcohol and cocaine). These results suggested a good long-term safety profile following the therapeutic use of ketamine in adolescence.

PMID 42928272
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PubMedChemMedChem2026-10-26

Synthesis of Nitrogen-Containing Heterocyclic Scaffolds and Applications in Scaffold Hopping: Development of an Aripiprazole Analog.

Alegbejo Price Temitayo Omowumi TO, Winant Pieterjan P, Júnior Paulo Eliandro da Silva PEDS, Melo Shaiani Maria Gil de SMG et al.

Heteroaromatic ring systems play a crucial role in drug development because they modulate physicochemical properties and expand the range of molecular interactions compared to non-heterocyclic aromatic rings. They are also widely represented among approved drugs. Among heteroatoms, nitrogen is the most prevalent in the diverse scaffold space of heterocyclic drugs, including those generated by fragment-based drug discovery approach. In this work, we show the synthesis of a set of novel or underexplored nitrogen heterocyclic fragments, obtained in three to five steps in moderate yields. In total, 12 fused [6,6] saturated/unsaturated bicycles were synthesized, which fulfill the general rule of fragment-like compounds. These heterocycles increased the fragment space of the CRAFT library and showed potential application in scaffold-hopping strategies for drug design. As a proof of concept, 2,6-naphthyridin-3-ol 2 was used to replace the 7-hydroxy-3,4-dihydroquinolin-2(1H)-one core of aripiprazole 41, generating 3-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2,6-naphthyridine 40, that effectively blocked cocaine-induced hyperactivity in rodents at 20 mg/kg without inducing catalepsy, displaying a pharmacological profile similar to aripiprazole and demonstrating promising antipsychotic potential.

PMID 42928417
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PubMedGels (Basel, Switzerland)2026-10-26

Insights into the Protonation State and Counterion Interactions of Linear Polyethyleneimine Materials.

Byrne Agustín J AJ, Vladimir Daniel D, Garro-Linck Yamila Y, Copello Guillermo J GJ et al.

Polyethyleneimine (PEI) polymers are widely used in the synthesis of nanoparticles, hydrogels and composite materials for biotechnological and environmental applications. However, the solid-state structural organization of linear PEI (L-PEI) materials, and how it is influenced by molecular weight, protonation state and counterion type, have not yet been comprehensively studied. In this work, solid-state nuclear magnetic resonance (ss-NMR), X-ray powder diffraction (XRD), small-angle X-ray scattering (SAXS) and time-domain NMR (TD-NMR) experiments were combined with theoretical calculations to analyze the local chemical environments, crystalline and nanoscale organization, and molecular mobility of L-PEI materials with different molecular weights. The analyzed materials were the free base (PEI·FB), the hydrochloride (PEI·HCl), the trifluoroacetate (PEI·TFA), and the sulfate-containing forms of L-PEI (PEI·Na2SO4 and PEI·H2SO4), as well as an intermediate protonation state obtained by the heterogeneous treatment with HCl-saturated isopropanol. Proton, 13C or 15N ss-NMR studies evidenced different chemical environments associated with changes in protonation state and counterion identity. Furthermore, XRD and SAXS showed that these variables, together with molecular weight and sample preparation conditions, influenced the crystalline arrangement and characteristic nanoscale organization of the polymer chains. Moreover, TD-NMR revealed the presence of three dynamically distinct proton populations, assigned to rigid, interfacial, and mobile domains, whose relative contributions and relaxation behavior varied among the PEI materials. Finally, high-resolution magic-angle spinning (HRMAS) NMR experiments were used to study different PEI-gel materials and films as well as the crosslinking of protonated PEI and sulfate ions.

PMID 42929946
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PubMedGels (Basel, Switzerland)2026-10-26

Dual-Drug Chitosan Hydrogel Loaded with Metformin and Cefazolin for Antibacterial, Anti-Inflammatory and Antioxidant Treatment of Drug-Resistant Bacteria-Infected Skin Wounds.

Zhang Yilin Y, Cao Jie J, Yan Yong Y, Li Zhaoyang Z et al.

Bacterial-infected skin wounds, especially those caused by drug-resistant pathogens accompanied by persistent inflammation, remain a major clinical therapeutic challenge. Rising antimicrobial resistance compromises the therapeutic effect of conventional single-agent antibiotics, creating an urgent demand for novel wound therapeutics that integrate bactericidal potency, immunomodulation and tissue regeneration capacity. In this work, an injectable multifunctional chitosan-based hydrogel (C@MC) was developed, which simultaneously incorporates metformin hydrochloride (as a potential antibiotic adjuvant) and cefazolin sodium (as a β-lactam class antibacterial drug). The optimized C@MC possesses interconnected three-dimensional pores with an initial storage modulus of ~0.83 kPa (C@MC360), featuring desirable mechanical strength, injectability, tissue adhesion and dual pH/glucose-responsive sustained drug release. In vitro evaluations revealed the dose-dependent bactericidal activity of C@MC against Staphylococcus aureus (S. aureus), Escherichia coli (E. coli) and New Delhi metallo-β-lactamase-1-producing E. coli (NDM-1 E. coli, resistant bacteria). The highest drug-laden group nearly eliminated all wound bacteria in vitro. It scavenged reactive oxygen species (ROS) to lower cellular MDA levels and suppress pro-inflammatory TNF-α and IL-6 in LPS-stimulated RAW 264.7 macrophages. In full-thickness mouse wounds infected with NDM-1 E. coli, C@MC360 achieved nearly complete wound closure, with only a 4.2% residual wound area on day 14, accompanied by suppressed inflammatory infiltration and accelerated wound regeneration. This dual-drug hydrogel integrates antibiotic potentiation, anti-inflammation and antioxidation, providing an intervention regimen for skin wounds infected with drug-resistant bacteria.

PMID 42929911
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PubMedResearch square2026-10-25

Activation of Trpv2 receptors increases the intravenous self-administration of low unit doses of cocaine in C3HeB/FeJ mice.

Applegate Devon T DT, Rahr Thomas R TR, Jentsch James David JD

Rationale Genetic variation contributes to individual differences in cocaine self-administration. Systems-genetics analyses identified Trpv2 as a candidate regulator of cocaine intake, with nucleus accumbens Trpv2 mRNA expression being negatively correlated with cocaine intake. Whether Trpv2 functionally regulates cocaine reinforcement remains unknown. Objectives We tested whether Trpv2 activation or inhibition affects cocaine self-administration. Methods Male NOD/ShiLtJ and male and female C3HeB/FeJ mice were trained to self-administer cocaine under a FR1 schedule. During responding at 0.5 mg/kg/infusion, mice received vehicle, the Trpv2 agonist O-1821, tranilast, or the selective Trpv2 antagonist SET2. A separate male and female C3HeB/FeJ cohort underwent dose-response testing at 0.1, 0.5, and 1.0 mg/kg/infusion following O-1821 or vehicle, with sex evaluated as a between-subject factor. Results NOD/ShiLtJ mice self-administered more cocaine than C3HeB/FeJ mice during acquisition. At a moderate dose of cocaine (0.5 mg/kg), neither Trpv2 activation nor antagonism altered cocaine intake in either strain. However, during dose-response testing, O-1821 increased cocaine intake at 0.1 mg/kg/infusion in C3HeB/FeJ mice in both sexes, along with significant sex-dependent reductions in cocaine intake with O-1821 at 0.5 and 1.0 mg/kg/infusion, respectively. Conclusions Genetic background and baseline variation in Trpv2 expression may contribute to individual differences in cocaine acquisition, whereas the acute effects of Trpv2 activation may depend on cocaine unit dose and sex. At low cocaine doses, Trpv2 activation may reduce reinforcement sensitivity and produce compensatory increases in intake. Trpv2 therefore warrants further investigation as a potential therapeutic target for substance use disorders.

PMID 42922708
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PubMedJournal of psychopharmacology (Oxford, England)2026-10-25

Combined muscarinic receptor M1 and M4 stimulation reverses cocaine-induced attention deficits in male mice.

Bornø Lærke L, Forsbøl Marie Søndergaard MS, Yüksel Oguzcan O, Bonnevie Veronika V et al.

Cocaine use and cocaine use disorder (CUD) are increasing public health concerns that lack effective treatments. CUD is a chronic illness characterized by relapse, altered activity in the prefrontal cortex and neurocognitive symptoms. Pharmacologically stimulating muscarinic acetylcholine receptors M1 and/or M4 has been shown to counteract abuse-related effects of cocaine and, independently, to have pro-cognitive effects. We tested the hypotheses that (1) withdrawal from a subchronic cocaine regimen in mice will negatively impact attention and impulsivity and (2) pharmacological stimulation of M1, M4, or M1 + M4 receptors will blunt or reverse these cocaine-induced impairments. Using a touchscreen rodent continuous performance test, male C57BL/6JRj mice were trained to respond to a target and withhold responses to a non-target stimulus. Mice received 20 mg/kg cocaine for 5 days and 30 mg/kg for 14 days. Then, the effect of treatment with the muscarinic M1 agonist VU0364572 (3.2 mg/kg) and the M4 PAM VU0152100 (1.8 mg/kg) was assessed in test probes challenging attention (variable stimulus duration) and impulsivity (variable intertrial interval), respectively. Cocaine exposure significantly and consistently impaired measures of attention (discriminability, accuracy), with less consistent effects on impulsivity (false alarm rate, premature responses). Treatment with combined VU0364572 + VU0152100 reversed cocaine-induced attention deficits, while each drug alone had little effect. These findings support the hypothesis that targeting M1 and M4 receptors can rescue cocaine-induced cognitive symptoms. Because cognitive impairments are thought to contribute to relapse to cocaine use, these results further support M1/M4 receptors as promising targets to treat CUD.

PMID 42921705
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