Delving into the Latest Updates on Isoprenaline Sulfate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [2]

Target

β1-adrenergic receptor x β2-adrenergic receptor

Action

agonists

Mechanism

β1-adrenergic receptor agonists(Beta-1 adrenergic receptor agonists), β2-adrenergic receptor agonists(Beta-2 adrenergic receptor agonists)

Therapeutic Areas

Immune System DiseasesRespiratory Diseases

Active Indication

Asthma

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC22H36N2O10S

InChIKeyZOLBALGTFCCTJF-UHFFFAOYSA-N

CAS Registry299-95-6

Background: During out-of-hospital cardiac arrest (OHCA), the patient presents with either a shockable or a non-shockable rhythm. Early cardiopulmonary resuscitation (CPR) and defibrillation of the shockable rhythm may increase chance of survival to more than 50%, however, if untreated, the heart rhythm will deteriorate to a non-shockable rhythm with dismal survival outcomes of 1-5%. Isoprenaline is a pro-arrhythmic drug used to treat bradycardia, and has a structural resemblance to epinephrine, which is the drug of choice during cardiac arrest with non-shockable rhythms.
Aims: To evaluate whether intravebous (IV) administration of isoprenaline increases the chance of return of spontaneous circulation (ROSC) to hospital arrival (main outcome) compared with IV epinephrine.
Study design: A randomized-controlled trial.
Setting: The study will be conducted in the Region of Southern Denmark, which has about 1.2 million inhabitants and an annual incidence of 1,200 OHCAs. The study will include bystander-witnessed patients with asystole at the arrival of the emergency medical services (EMS). Randomization will take place on arrival of the EMS, where the OHCA patients randomly will be assigned to receive an intravenous injection of isoprenaline (600 µg) or an intravenous injection of adrenaline (1 mg) in a 1:1 ratio. The study will include 1,178 OHCAs over a time period of about 3.5 years.

Start Date01 Mar 2025

Sponsor / Collaborator

University of Southern Denmark

[+1]

ISRCTN17309312

/ CompletedNot ApplicableIIT

Isoprenaline infusion as a method of induction of Atrial Fibrillation: a randomised controlled trial investigating the use of Isoprenaline to induce an episode of atrial fibrillation

Start Date05 Jan 2015

Sponsor / Collaborator-

100 Clinical Results associated with Isoprenaline Sulfate

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100 Translational Medicine associated with Isoprenaline Sulfate

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100 Patents (Medical) associated with Isoprenaline Sulfate

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681

Literatures (Medical) associated with Isoprenaline Sulfate

01 Dec 2024·Pest Management Science

Design, synthesis and antimicrobial activity of novel berberine derivatives

Article

Author: Liu, Ying‐Qian ; Ma, Li ; Jin, Ya‐Rui ; Li, Fu‐Ping ; Zhang, Bao‐Qi ; Chen, Gui‐Sha ; Mou, Guo‐Liang ; Jing, Cheng‐Xin ; Qin, Lu‐Lu ; Wang, Deng‐Tuo ; Zhang, Zhi‐Jun ; An, Jun‐Xia

AbstractBACKGROUNDThe threats to the safety of humans and the environment and the resistance of agricultural chemicals to plant pathogenic fungi and bacteria highlight an urgent need to find safe and efficient alternatives to chemical fungicides and bactericides. In this study, a series of Berberine (BBR) derivatives were designed, synthesized and evaluated for in vitro and in vivo antimicrobial activity against plant pathogenic fungi and bacteria.RESULTSBioassay results indicated that compounds A11, A14, A20, A21, A22, A25, A26, E1, E2, E3, Z1 and Z2 showed high inhibitory activity against Sclerotinia sclerotiorum and Botrytis cinerea. Especially, A25 showed a broad spectrum and the highest antifungal activity among these compounds. Its EC50 value against Botrytis cinerea was 1.34 μg mL−1. Compound E6 possessed high inhibitory activity against Xanthomonas oryzae and Xanthomonas Campestris, with MIC90 values of 3.12 μg mL−1 and 1.56 μg mL−1. A Topomer CoMFA model was generated for 3D‐QSAR studies based on anti‐B. cinerea effects, with high predictive accuracy, showed that the addition of an appropriate substituent group at the para‐position of benzyl of BBR derivatives could effectively improve the anti‐B. cinerea activity. In addition, compound A25 could significantly inhibit the spore germination of Botrytis cinerea at low concentration, and compound F4 exhibited remarkable curative and protective efficiencies on rice bacterial leaf blight.CONCLUSIONThis study indicates that the BBR derivatives are hopeful for further exploration as the lead compound with novel antimicrobial agents. © 2024 Society of Chemical Industry.

06 Nov 2024·Journal of Agricultural and Food Chemistry

Novel “Phenyl-Pyrazoline-Oxadiazole” Ternary Substructure Derivatives: Synthesis, Insecticidal Activities, and Structure–Activity Relationship Study

Article

Author: Guo, Renjiang ; Ma, Xining ; Tian, Bihong ; Tu, Hong ; Wu, Jian ; Tao, Jiaxu ; Yang, Zhaokai

In recent years, isoxazole insecticides or parasiticides targeting the γ-aminobutyric acid receptor, such as fluralaner or fluxametamide, featured a novel chemical structure and exhibited potent insecticidal activity with no-cross resistance. Thus, many research institutes have tried to modify the structures of these agents to find a new insecticide. Previously, the majority of researchers stuck to the "phenyl-isoxazole-phenyl" structure, making modifications only to other components. In this study, the "phenyl-isoxazole-phenyl" ternary motif was modified for the first time based on bioisosterism theory. A series of new derivatives carrying pyrazoline and 1,3,4-oxadiazole moieties were designed and synthesized to investigate their insecticidal activities against the diamondback moth (Plutella xylostella) and fall armyworm (Spodoptera frugiperda). Preliminary bioassay data showed that some of the target compounds exhibited good insecticidal activities against P. xylostella and S. frugiperda. Especially, compound A21 showed insecticidal activity against P. xylostella (LC₅₀ = 1.2 μg/mL) better than commercial insecticide ethiprole (LC₅₀ = 2.9 μg/mL) but worse than parasiticide fluralaner (LC₅₀ = 0.5 μg/mL). Similarly, compound A21 exhibited insecticidal activity to S. frugiperda (LC₅₀ = 13.2 μg/mL) better than commercial insecticide fipronil (LC₅₀ = 78.8 μg/mL) but worse than fluralaner (LC₅₀ = 0.7 μg/mL). Compound A21 could serve as a potential lead compound to control P. xylostella and S. frugiperda. The three-dimensional quantitative structure-activity relationship model revealed that the further introduction of an electron-donating group in the 2- or 3-site may increase the insecticidal activity of A21. Molecular dynamics simulations showed that the hydrogen bond of A21 and receptor was important for the binding receptor. This study has identified a new substructure called "phenyl-pyrroline-oxadiazole" instead of the previously known "phenyl-isoxazole-phenyl" substructure, offering a useful guide for the design of novel insecticide molecules.

01 Nov 2024·Pesticide Biochemistry and Physiology

Scaffold hopping approach to the novel hexacyclic pyrazol-3-amide derivatives as potential multi-target insect growth regulators candidates

Article

Author: Guo, Bingbo ; Yang, Qing ; Yang, Xinling ; Chen, Lei ; Cao, Congwang ; Luo, Shihui ; Wang, Chunying ; Feng, Yanjiao ; Zhang, Li

Ecdysone receptor (EcR) and three insect chitinases (OfChtI, OfChtII, and OfChi-h) are considered as attractive targets for the development of novel insect growth regulators (IGRs) since they are closely related to the insect molting. In this study, to develop potent multi-target IGRs, a series of hexacyclic pyrazol-3-amide derivatives were rationally designed by utilizing the scaffold hopping strategy with the previously reported compound 6j (N-(4-bromobenzyl)-2-phenyl-4,5,6,7-tetrahydro-2H-indazole-5-carboxamide) as a lead compound. The bioassay results indicated that most of the target compounds exhibited obvious insecticidal activity. Especially, compounds a5 and a21 displayed excellent insecticidal activities against P. xylostella with LC₅₀ values of 82.29 and 69.45 mg/L, respectively, exceeding that of 6j (263.78 mg/L). Compounds a5 and a21 also dramatically disturbed the growth and development of O. furnacalis larvae, and their LC₅₀ values were 124.71 and 127.54 mg/L, respectively, superior to the lead 6j (267.33 mg/L). The action mechanism study revealed that the most active compound a21 could act simultaneously on EcR (21.4 % binding activity at 8 mg/L), OfChtI (94.9 % inhibitory at 10 μM), OfChtII (23.1 % inhibitory at 10 μM), and OfChi-h (94.3 % inhibitory at 10 μM), significantly higher than that of the lead compound 6j. The result of molecular docking indicated that transferring the carboxamide group from pyrazole position 5 to 3 enhanced the interactions of a21 with the key amino acid residues of the OfChtI, OfChtII, and OfChi-h, resulting in stronger affinity to the three targets than 6j. The present work offers a useful guidance for the further development of novel multi-target IGRs.

100 Deals associated with Isoprenaline Sulfate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Isoprenaline Sulfate	R03AB02	DB01064

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Asthma	China	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESC2016	Not Applicable	estradiol	-	Vehicle	gtjjfnxhgj(lbceewmosg) = uteauwcmii dzpwhuwhjc (xhbkecfmby ) View more	-	29 Aug 2016
				Beta-estradiol	gtjjfnxhgj(lbceewmosg) = rvwiweggxa dzpwhuwhjc (xhbkecfmby ) View more
Pubmed \| Heart	Not Applicable	-	-	Atropine	yltsigdnej(rfweyoteuc) = dlacyyztvt sgglwxcuek (wrsmdlmnwk )	-	01 Mar 1989
				Isoprenaline	yltsigdnej(rfweyoteuc) = cyamxgunlx sgglwxcuek (wrsmdlmnwk )