Nylidrin hydrochloride
(Synonyms: 布芬宁盐酸盐,Buphenine hydrochloride) 目录号 : GC39414
An agonist of β-ARs and antagonist of NR1A/2B subunit-containing NMDA receptors
Cas No.:849-55-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nylidrin is an agonist of β-adrenergic receptors and antagonist of NR1A/2B subunit-containing NMDA receptors.1,2 It binds to β-adrenergic receptors (Kd = 0.37 ?M) and activates adenylate cyclase with a Ka value of 1.3 ?M.1 Nylidrin is selective for NR1A/2B over NR1A/2A and NR1A/2C subunit-containing NMDA receptors (IC50s = 0.18, 32, and 42 ?M, respectively, for the recombinant receptors expressed in Xenopus oocytes).2 It inhibits NMDA-induced currents in primary rat cortical neurons (IC50 = 0.22 ?M). It also decreases blood pressure and increases heart rate in spontaneously hypertensive rats (SHRs) with a minimum effective dose (MED) of 0.5 mg/kg.3 Nylidrin (20 and 100 ?M) inhibits influenza hemagglutinin 2-mediated membrane fusion in Vero E6 cells.4 It inhibits infection of MDCK cells by H1N1 and H3N2 influenza isolates in vitro (EC50s = 7.2 and 12.1 ?M, respectively) and prevents infection in a mouse model of mouse-adapted H1N1 infection.
1.Bilezikian, J.P., Dornfeld, A.M., and Gammon, D.E.Structure-binding-activity analysis of beta-adrenergic amines—I. Binding to the beta receptor and activation of adenylate cyclaseBiochem. Pharmacol.27(10)1445-1454(1978) 2.Whittemore, E.R., Ilyin, V.I., Konkoy, C.S., et al.Subtype-selective antagonism of NMDA receptors by nylidrinEur. J. Pharmacol.337(2-3)197-208(1997) 3.Yen, T.T., and Pearson, D.V.Nylidrin: A potent antihypertensive agent in hypertensive ratsRes. Commun. Chem. Pathol. Pharmacol.23(1)11-28(1979) 4.Jang, Y., Shin, J.S., Lee, J.-Y., et al.In vitro and in vivo antiviral activity of nylidrin by targeting the hemagglutinin 2-mediated membrane fusion of influenza A virusViruses12(5)581(2020)
| Cas No. | 849-55-8 | SDF | |
| 别名 | 布芬宁盐酸盐,Buphenine hydrochloride | ||
| Canonical SMILES | OC(C(NC(C)CCC1=CC=CC=C1)C)C2=CC=C(O)C=C2.[H]Cl | ||
| 分子式 | C19H26ClNO2 | 分子量 | 335.87 |
| 溶解度 | DMSO: ≥ 41 mg/mL (122.07 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9773 mL | 14.8867 mL | 29.7734 mL |
| 5 mM | 0.5955 mL | 2.9773 mL | 5.9547 mL |
| 10 mM | 0.2977 mL | 1.4887 mL | 2.9773 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Antiallergic activity of Nylidrin hydrochloride (RHC 3432-A). II. A lack of correlation between inhibition of mediator release and levels of cyclic AMP
Int Arch Allergy Appl Immunol 1983;70(4):303-10.PMID:6186609doi
Nylidrin hydrochloride has weak beta-adrenergic agonist properties with rat mast cells, and shows synergy with 3-isobutyl-1-methylxanthine (IBMX) in raising intracellular cAMP in purified mast cells; both of these properties can be blocked by dl-propranolol. However, the action of Nylidrin hydrochloride as an inhibitor of histamine secretion from purified rat mast cells is not antagonized by dl-propranolol, nor is it potentiated by IBMX. Nylidrin-induced elevation of cellular cAMP in purified rat mast cells shows no correlation with nylidrin-induced inhibition of histamine release. Thus, Nylidrin hydrochloride inhibits release of histamine from mast cells by a novel, non-adrenergic mechanism, which is not dependent on increased levels of cAMP.
Antiallergic activity of Nylidrin hydrochloride (RHC 3432-A). I. Effect on release of histamine in vitro from rat peritoneal mast cells, guinea pig lung slices and human basophils
Int Arch Allergy Appl Immunol 1983;70(4):295-302.PMID:6186608doi
Nylidrin (RHC 3432-A) has been investigated for its antiallergic activity in three in vitro models. Nylidrin was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guinea pig lung slices. The inhibition of the release of histamine by nylidrin in all three models was not antagonized by propranolol, indicating that nylidrin does not inhibit histamine release via stimulation of beta-adrenergic receptors. Isoproterenol and epinephrine were effective as inhibitors of the release of histamine only from guinea pig lung while salbutamol and terbutaline had no effect on immunologic release of histamine in all three models. Detailed comparative studies with disodium cromoglycate (DSCG) indicated that the mechanism of action of nylidrin in the rat mast cell model is different from that of DSCG.
Efficacy of Nylidrin hydrochloride in the treatment of cognitive impairment in the elderly
J Am Geriatr Soc 1979 May;27(5):235-6.PMID:372292DOI:10.1111/j.1532-5415.1979.tb06039.x.
A double-blind study was conducted on the effects of Nylidrin hydrochloride versus placebo in 60 patients with mild to moderate symptoms of chronic brain syndrome. Their ages ranged from 65 to 99 years. Preliminary results indicated that nylidrin HCl (a vasodilator) is a relatively safe therapeutic agent and more effective than placebo in ameliorating the symptoms of cognitive impairment associated with aging, on both a short term (3-month) and a long-term (9-month) basis. In a dosage of 24 mg daily, it reached its peak effectiveness after 3 months of use.
High-performance liquid chromatography of two peripheral vasodilators, Nylidrin hydrochloride and isoxsuprine hydrochloride, in pharmaceutical dosage forms
J Pharm Sci 1979 Oct;68(10):1264-7.PMID:512857DOI:10.1002/jps.2600681018.
A reliable and selective high-pressure liquid chromatographic (HPLC) procedure for the quantitative determination of Nylidrin hydrochloride or isoxsuprine hydrochloride in pharmaceutical dosage forms is described. The specificity of the stability-indicating HPLC procedure is presented for Nylidrin hydrochloride.
Pentoxifylline for intermittent claudication
Cochrane Database Syst Rev 2015 Sep 29;9(9):CD005262.PMID:26417854DOI:10.1002/14651858.CD005262.pub3.
Background: Intermittent claudication (IC) is a symptom of peripheral arterial disease (PAD) and is associated with high morbidity and mortality. Pentoxifylline, one of many drugs used to treat IC, acts by decreasing blood viscosity, improving erythrocyte flexibility and promoting microcirculatory flow and tissue oxygen concentration. Many studies have evaluated the efficacy of pentoxifylline in treating individuals with PAD, but results of these studies are variable. This is an update of a review first published in 2012. Objectives: To determine the efficacy of pentoxifylline in improving the walking capacity (i.e. pain-free walking distance and total (absolute, maximum) walking distance) of individuals with stable intermittent claudication, Fontaine stage II. Search methods: For this update, the Cochrane Vascular Group Trials Search Co-ordinator searched the Specialised Register (last searched April 2015) and the Cochrane Register of Studies (2015, Issue 3). Selection criteria: All double-blind, randomised controlled trials (RCTs) comparing pentoxifylline versus placebo or any other pharmacological intervention in patients with IC Fontaine stage II. Data collection and analysis: Two review authors separately assessed included studies,. matched data and resolved disagreements by discussion. Review authors assessed the methodological quality of studies by using the Cochrane 'Risk of bias' tool and collected results related to pain-free walking distance (PFWD) and total walking distance (TWD). Comparison of studies was based on duration and dose of pentoxifylline. Main results: We included in this review 24 studies with 3377 participants. Seventeen studies compared pentoxifylline versus placebo. In the seven remaining studies, pentoxifylline was compared with flunarizine (one study), aspirin (one study), Gingko biloba extract (one study), Nylidrin hydrochloride (one study), prostaglandin E1 (two studies) and buflomedil and nifedipine (one study). The quality of the evidence was generally low, with large variability in reported findings.. Most included studies did not report on random sequence generation and allocation concealment, did not provide adequate information to allow selective reporting to be judged and did not report blinding of assessors. Heterogeneity between included studies was considerable with regards to multiple variables, including duration of treatment, dose of pentoxifylline, baseline walking distance and participant characteristics; therefore, pooled analysis was not possible.Of 17 studies comparing pentoxifylline with placebo, 14 reported TWD and 11 reported PFWD; the difference in percentage improvement in TWD for pentoxifylline over placebo ranged from 1.2% to 155.9%, and in PFWD from -33.8% to 73.9%. Testing the statistical significance of these results generally was not possible because data were insufficient. Most included studies suggested improvement in PFWD and TWD for pentoxifylline over placebo and other treatments, but the statistical and clinical significance of findings from individual trials is unclear. Pentoxifylline generally was well tolerated; the most commonly reported side effects consisted of gastrointestinal symptoms such as nausea. Authors' conclusions: Given the generally poor quality of published studies and the large degree of heterogeneity evident in interventions and in results, the overall benefit of pentoxifylline for patients with Fontaine class II intermittent claudication remains uncertain. Pentoxifylline was shown to be generally well tolerated.Based on total available evidence, high-quality data are currently insufficient to reveal the benefits of pentoxifylline for intermittent claudication.