Pharmacological Profile of ZK 96 480, a New Chemically and Metabolically Stable Prostacyclin Analogue with Oral Availability and High PGI2 Intrinsic Activity

2015 ◽  
pp. 485-491 ◽  
Author(s):  
C. St. St�rzebecher ◽  
M. Haberey ◽  
B. M�ller ◽  
E. Schillinger ◽  
G. Schr�der ◽  
...  
Keyword(s):  
Intrinsic Activity ◽  
Pharmacological Profile ◽  
Prostacyclin Analogue ◽  
Oral Availability

The in vitro pharmacological profile of TD-5108, a selective 5-HT4 receptor agonist with high intrinsic activity

2008 ◽  
Vol 378 (1) ◽  
pp. 125-137 ◽  
Author(s):  
J. A. M. Smith ◽  
D. T. Beattie ◽  
D. Marquess ◽  
J.-P. Shaw ◽  
R. G. Vickery ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Intrinsic Activity ◽  
Pharmacological Profile

scholarly journals Synthesis and Evaluation of the Antidepressant-like Properties of HBK-10, a Novel 2-Methoxyphenylpiperazine Derivative Targeting the 5-HT1A and D2 Receptors

2021 ◽  
Vol 14 (8) ◽  
pp. 744
Author(s):  
Kinga Sałaciak ◽  
Natalia Malikowska-Racia ◽  
Klaudia Lustyk ◽  
Agata Siwek ◽  
Monika Głuch-Lutwin ◽  
...  
Keyword(s):  
Forced Swim Test ◽  
Chronic Administration ◽  
Tail Suspension Test ◽  
D2 Receptors ◽  
Intrinsic Activity ◽  
Pharmacological Profile ◽  
Behavioral Experiments ◽  
Number Of Patients

The increasing number of patients reporting depressive symptoms requires the design of new antidepressants with higher efficacy and limited side effects. As our previous research showed, 2-methoxyphenylpiperazine derivatives are promising candidates to fulfill these criteria. In this study, we aimed to synthesize a novel 2-methoxyphenylpiperazine derivative, HBK-10, and investigate its in vitro and in vivo pharmacological profile. After assessing the affinity for serotonergic and dopaminergic receptors, and serotonin transporter, we determined intrinsic activity of the compound at the 5-HT1A and D2 receptors. Next, we performed behavioral experiments (forced swim test, tail suspension test) to evaluate the antidepressant-like activity of HBK-10 in naïve and corticosterone-treated mice. We also assessed the safety profile of the compound. We showed that HBK-10 bound strongly to 5-HT1A and D2 receptors and presented antagonistic properties at these receptors in the functional assays. HBK-10 displayed the antidepressant-like effect not only in naïve animals, but also in the corticosterone-induced mouse depression model, i.e., chronic administration of HBK-10 reversed corticosterone-induced changes in behavior. Moreover, the compound’s sedative effect was observed at around 26-fold higher doses than the antidepressant-like ones. Our study showed that HBK-10 displayed a favorable pharmacological profile and may represent an attractive putative treatment candidate for depression.

Substrate specificity and inducibility of TACE (tumour necrosis factor α-converting enzyme) revisited: the Ala-Val preference, and induced intrinsic activity

2003 ◽  
Vol 70 ◽  
pp. 39-52 ◽  
Author(s):  
Roy A. Black ◽  
John R. Doedens ◽  
Rajeev Mahimkar ◽  
Richard Johnson ◽  
Lin Guo ◽  
...  
Keyword(s):  
Substrate Specificity ◽  
Recent Work ◽  
Tumour Necrosis Factor ◽  
Tumour Necrosis ◽  
Transforming Growth Factor ◽  
Intrinsic Activity ◽  
Converting Enzyme ◽  
Tumour Necrosis Factor Α ◽  
Factor Α ◽  
Necrosis Factor

Tumour necrosis factor α (TNFα)-converting enzyme (TACE/ADAM-17, where ADAM stands for a disintegrin and metalloproteinase) releases from the cell surface the extracellular domains of TNF and several other proteins. Previous studies have found that, while purified TACE preferentially cleaves peptides representing the processing sites in TNF and transforming growth factor α, the cellular enzyme nonetheless also sheds proteins with divergent cleavage sites very efficiently. More recent work, identifying the cleavage site in the p75 TNF receptor, quantifying the susceptibility of additional peptides to cleavage by TACE and identifying additional protein substrates, underlines the complexity of TACE-substrate interactions. In addition to substrate specificity, the mechanism underlying the increased rate of shedding caused by agents that activate cells remains poorly understood. Recent work in this area, utilizing a peptide substrate as a probe for cellular TACE activity, indicates that the intrinsic activity of the enzyme is somehow increased.

In silico ADME, Bioactivity and Toxicity Parameters Calculation of Some Selected Anti-Tubercular Drugs

2016 ◽  
Vol 6 (6) ◽  
pp. 77 ◽  
Author(s):  
Shashank Shekhar Mishra ◽  
Chandra Shekhar Sharma ◽  
Hemendra Pratap Singh ◽  
Harshda Pandiya ◽  
Neeraj Kumar
Keyword(s):  
Antibiotic Resistance ◽  
In Silico ◽  
Bacillus Calmette Guerin ◽  
Computational Investigation ◽  
Pharmacological Profile ◽  
In Silico Toxicity ◽  
Is Development ◽  
Potent Drug ◽  
Minimal Resistance ◽  
Parameters Calculation

Tuberculosis, one of the most frequent infectious diseases, is caused by a mycobacterium tuberculosis bacteria and it infects several hundred million people each year, results in several million deaths annually. Because there is development of antibiotic resistance, the disease becomes incurable. So, in the absence of effective and potent drug with minimal resistance problems, the mortality rate increases annually. In this computational investigation, we performed In-silico ADME, bioactivity and toxicity parameters calculation of some selected anti-tuberculosis agents. To design a new molecule having good pharmacological profile, this study will provide the lead information.Key Words: Tuberculosis (TB), Bacillus Calmette-Guerin vaccine, TPSA, In Silico toxicity

An Overview on Phytochemical and Pharmacological Profile of Morus alba Linn.

2020 ◽  
Vol 16 ◽  
Author(s):  
Arpita Paul ◽  
Monami Rajiung ◽  
Kamaruz Zaman ◽  
Sushil Kumar Chaudhary ◽  
Hans Raj Bhat ◽  
...  
Keyword(s):  
Traditional Medicine ◽  
Morus Alba ◽  
Biologically Active ◽  
Pharmacological Profile ◽  
Pharmacological Activities ◽  
Significant Information ◽  
The Past ◽  
Comprehensive Information ◽  
The Family ◽  
White Mulberry

Background: Morus alba Linn. commonly known as white mulberry, belongs to the family Moraceae, is a promising traditional medicine. In Asia, besides its use in the preparation of delicacies, every part of this plant is utilized in traditional medicine. Over the past decade, studies related to identification and isolation of biologically active compounds, with flavonoids as the major class of phytoconstituents, from this plant has been reported. These phytoconstituents are not only found to be beneficial for the maintenance of general health but also are associated with a range of potential pharmacological activities such as antioxidant, anti-inflammatory, anti-diabetic, anticancer, hepatoprotective, cardioprotective, neuroprotective to name a few. Objective: This review aims to provide upgraded and comprehensive information regarding the phytochemical, ethnomedicinal use and pharmacological profile of the plant Morus alba Linn. Method: The significant information has been collected through various database viz. PubMed, Scopus, Web of Science, Science Direct based on the recent findings, using different terms of Morus alba. Results: The outcome of the study suggests that Morus alba is a multifunctional plant numerous phytochemicals, and possess a range of pharmacological activities. Conclusion: The data assembled on Morus alba will be beneficial to trigger research in various fields of pharmaceutical and allied science to explore the medicinal importance of this unique plant.

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