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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

PubMedPsychopharmacology2026-09-10

Neuropharmacology of levamisole and its phase I metabolites: lack of evidence for levamisole-cocaine interactions.

Zolkowska Dorota D, Lehner Kurt R KR, Partilla John S JS, Blough Bruce E BE et al.

The anthelmintic agent, levamisole, is a cocaine adulterant that causes serious adverse effects in humans. A number of hypotheses have been proposed to explain why levamisole is used as an adulterant. Here, we examined whether levamisole might enhance acute pharmacological effects of cocaine. Levamisole and its phase I metabolites were tested for in vitro activity at monoamine receptors and transporters. The effect of levamisole (0.1-10 µM) on cocaine-induced inhibition of [3H]dopamine uptake was examined in rat brain synaptosomes. In vivo microdialysis in nucleus accumbens of male rats was employed to determine neurochemical effects of cocaine (1-3 mg/kg, intravenous), in the absence or presence of levamisole (1:1 ratio with cocaine). Levamisole displayed no measurable activity at monoamine receptors or transporters. The metabolite aminorex acted as a potent substrate at transporters for dopamine, norepinephrine and serotonin, whereas rexamino had affinity for adrenoreceptors and weak substrate activity at norepinephrine transporters. Levamisole did not alter cocaine-induced inhibition of dopamine uptake in vitro. Administration of cocaine, or cocaine plus levamisole, produced similar increases in extracellular dopamine and locomotor stimulation in vivo. We found no evidence that levamisole alters the acute pharmacological effects of cocaine in male rats. The metabolite aminorex is a potent monoamine transporter substrate which could contribute to effects of levamisole under certain conditions (e.g., repeated, high-dose exposure), but most studies in human users of levamisole-adulterated cocaine have failed to detect measurable quantities of aminorex.

PMID 42717004
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PubMedFrontiers in pediatrics2026-09-10

Diagnostic challenges in infant death associated with maternal cocaine abuse during pregnancy and lactation: a forensic case report and review of the literature.

Iacoponi Naomi N, Maggi Rebecca R, Nardini Vincenzo V, Chericoni Silvio S et al.

Maternal cocaine abuse during pregnancy and lactation represents a critical public health crisis. Recent 2024-2025 data indicate approximately 4.3 million users in the United States and 2.7 million young adults in Europe. While epidemiological evidence suggests an independent association between prenatal cocaine exposure and Sudden Infant Death Syndrome (SIDS), forensic interpretation remains complex due to the lack of validated toxicological thresholds for the pediatric population. We report the case of a 36-day-old infant who died suddenly and unexpectedly. Post-mortem investigations were performed to differentiate between SIDS and toxicological intoxication. Forensic hair analysis confirmed chronic cocaine exposure, occurring both in utero and via lactation. A systematic review of the literature was conducted in accordance with the PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines. The search focused on fetal and infant fatalities associated with maternal cocaine consumption to identify recurrent toxicological patterns. The systematic review identified seven key studies describing neonatal deaths linked to maternal cocaine use. A significant discrepancy was observed between adult post-mortem concentrations, ranging from 900 ng/mL in cardiac-related deaths to over 19,000 ng/mL in acute intoxications, and neonatal levels, which showed mean concentrations of 39 ng/mL, though extreme cases have reached 4.8 mg/dL. This variability underscores the difficulty in establishing a lethal range for infants. The findings highlight a critical gap in forensic pathology and toxicology. There is an urgent need for systematic data collection during autopsies to establish standardized reference intervals. Improving these datasets is essential for forensic pathologists to accurately distinguish between incidental exposure and cocaine-induced fatality in pediatric cases.

PMID 42718795
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PubMedJournal of medicinal chemistry2026-09-10

A Series of Aryl-Substituted-(biphenyl)methyl-sulfinylmethylthiazoles as Novel and Atypical Dopamine Transporter Inhibitors.

Camacho-Hernandez Gisela A GA, Cao Jianjing J, Okorom Amarachi A, Straub Carolyn J CJ et al.

Dependence on psychostimulants, including cocaine and methamphetamine, is driving the fourth wave of U.S. drug overdoses. The search for atypical dopamine transporter (DAT) inhibitors for the treatment of psychostimulant use disorders has identified both structurally and pharmacologically diverse compounds that bind DAT but do not produce cocaine-like behaviors in experimental animals. Nevertheless, low binding affinity at hDAT, metabolic instability and high potency in the human ether-à-go-go-related gene (hERG) channel have limited further development. Herein, we describe the synthesis of a novel series of aryl-substituted-(biphenyl)methyl-sulfinylmethylthiazoles and identify two lead molecules, 32b and 39b that bind hDAT (Ki = 63.0 and 78.5 nM, respectively) and have hERG channel activities predicted to be in the low μM range. Despite demonstrated brain penetrability and target engagement neither compound produced cocaine-like locomotor stimulation or conditioned place preference, in mice, thus representing a new class of atypical DAT inhibitors and potential leads for pharmacotherapeutic development.

PMID 42720470
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PubMedSmall (Weinheim an der Bergstrasse, Germany)2026-09-10

Manipulating the Buried Interfacial Dipole: The Role of Pyridine Acetate-Hydrochloride Isomers in Carbon-Based Perovskite Solar Cells Prepared in Air.

Shi Yifei Y, Gong Jianwen J, Wang Xu X, Hu Shuming S et al.

The buried interface between tin oxide and perovskite is the key factor for non-radiative recombination and energy level mismatch, which limits the performance and stability of perovskite solar cells. This work explores a simple interfacial dipole engineering strategy, where three pyridine acetate-hydrochloride (PAH) isomer molecules (2-PAH, 3-PAH, and 4-PAH) are used to modify the SnO2 electron transport layer. The 3-PAH-modified layer can control the work function of tin oxide, achieve the best energy level alignment, and improve the crystallization quality of the perovskite film, thereby effectively suppressing interface recombination and promoting electron extraction. All the devices are prepared in air, and the device optimized by 3-PAH achieved a champion energy conversion efficiency of 14.31% and demonstrated stability. Subsequent to an 800 h placement in an N2 glove box or a 340 h exposure to an air environment, the unencapsulated target devices that were modified by 3-PAH maintained 80.7% and 81.3% of their initial efficiency.

PMID 42717680
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PubMedAAPS PharmSciTech2026-09-10

Ethosomal Gel-Based Topical Delivery of Albendazole Hydrochloride for Psoriasis: In Vitro and In Vivo Evaluation.

Rençber Seda S, Karpuz Merve M, Ünlü Çakıcı Büşra B, Karayıldırım Çinel Köksal ÇK et al.

This study aimed to develop an albendazole hydrochloride (ALB)-loaded ethosomal gel for topical psoriasis treatment. ALB-loaded ethosomes were prepared and characterized to select the optimal formulation, which was subsequently incorporated into an HPMC-based hydrogel. The ethosomal gel was evaluated through physicochemical, in vitro and in vivo studies. The optimized ethosomal formulation prepared by the film hydration method exhibited a mean vesicle size of 490.00 ± 0.14 nm, polydispersity index of 0.31 ± 0.14, zeta potential of -22.85 ± 2.28 mV and encapsulation efficiency of 23.90 ± 1.43%. After incorporation into the hydrogel matrix, the Gel4-E3/ALB formulation demonstrated appropriate mechanical properties (hardness 8.42 ± 0.70 mN, adhesiveness - 16.85 ± 1.50 mN·s, elasticity 0.89 ± 0.07, cohesiveness 1.14 ± 0.09) and shear-thinning behavior, ensuring ease of application and skin retention. A controlled release pattern was observed, consistent with the controlled-release behavior expected from ethosomal hydrogel systems. Radiolabeling studies demonstrated high labeling efficiency (> 95%). In vitro cytotoxicity evaluation indicated that the optimized ethosomal gel formulation was non-toxic. In vivo studies performed in an imiquimod (IMQ)-induced psoriatic mouse model revealed significant therapeutic improvement in the Gel4-E3/ALB-treated group compared with the IMQ control, with visible reduction in erythema, scaling, and skin thickening after the fifth day of treatment. Hematological analysis showed no adverse effects associated with the formulation. Histopathological evaluation confirmed the reduction in epidermal hyperplasia and inflammatory cell infiltration in the treated group. The developed ALB-loaded ethosomal gel represents a safe and promising topical therapeutic system for psoriasis management.

PMID 42717176
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PubMedEpidemiologia e servicos de saude : revista do Sistema Unico de Saude do Brasil2026-09-10

Hepatitis A among people experiencing homelessness: a case series, Curitiba, Paraná State, Brazil, 2023-2024.

Silva Janilza Silveira JS, de Carvalho Renata Barbosa Vilaça Marques RBVM, de Oliveira Alcides Souto AS, Dos Santos Diego Spinoza DS et al.

To describe hepatitis A cases among people experiencing homelessness in Curitiba, Paraná State, Brazil, in 2023-2024. This case series included people experiencing homelessness who were reported with hepatitis A in the Notifiable Diseases Information System between November 1, 2023, and May 29, 2024, in Curitiba. This population was identified by reviewing electronic medical records and the registry database of the Consultório na Rua [Street Outreach Clinic] team. Sociodemographic, clinical, and laboratory variables were extracted. Of 281 reported cases, 18 (6.4%) occurred among individuals experiencing homelessness; 16 were male. The mean age was 31±7 years. Regarding substance use in this population, 17 individuals reported crack cocaine use and 14 reported alcohol use. Mean aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels were 1,290.94 (±1,144.82) U/L and 1,558.13 (±1,050.00) U/L, respectively. The mean total bilirubin level at clinical presentation was 5.29 (±3.59) mg/dL, and jaundice was present in 55.6% of cases. Two deaths were recorded among the 18 cases in individuals experiencing homelessness (mortality: 11.1%), compared with three deaths among the remaining 263 reported cases (mortality: 1.1%). Symptoms of acute liver failure were observed in hepatitis A cases among people experiencing homelessness, all of whom required hospitalization; deaths were also reported.

PMID 42718314
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