Study of Beta-adre Oreceptor Blocki G a D a Tihyperte Sive Activity of a Ewly Sy Thesized Aryloxypropa Olami E Derivative, Pp-28 I Laboratory a Imals

نویسندگان

  • Aakanksha Dube
  • Sumit Chaudhary
  • Poonam Piplani
چکیده

Beta-adrenoceptor blockers are an important class of drugs used in management of patient with cardiovascular diseases. These drugs have been shown to reduced mortility in hypertension. However, the main side effect of these drugs is due to antagonism of β2adrenoceptors in the airways, resulting in bronchospasm. Therefore, more cardio selective betablockers have been developed to offer a lower side effect profile. We have studied a new aryloxypropanolamine derivative (PP-28) with more cardio selectivity and efficacy against hypertension in rats. Oxalate salts of 1-tert-butylamino-3-[3-(tert-butylamino-methyl)-phenoxy]propan-2-ol. (PP-28) is a novel beta-adrenoceptor antagonist. In-vitro studies in rat isolated right atria, rat uterus and rat distal colon preparations were carried out to investigate the potency of PP-28 towards different beta-adrenoceptor subtypes. The pA2 values of PP-28 for β1, β2, and β3 adrenoceptor were 7.69+/-0.10, 6.03+/-0.08 and 6.10+/-0.14, respectively. The β1/ β2 selectivity ratio calculated was in the order of PP-28 > atenolol > propranolol. PP-28 also blocked significantly isoprenaline induced tachycardia and hypotensive responses in anesthetized rat.Antihypertensive effect of PP-28 was observed in left renal artery ligated (LRA) and 10% Fructose induce hypertensive rat.Treatment with PP-28 (1, 3 and 10 mg/kg, orally) produced a dose dependent decrease in MAP and heart rate of LRA ligated rats as well as 10% Fructose induce hypertensive rat .The efficacy of PP-28 was found to be greater then atenolol. In conclusion, PP-28 is a cardioselective beta-adrenoceptor antagonist, possessing potent Antihypertensive effects in left renal artery ligated and 10% Fructose induce hypertensive rat

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Amitraz Poisoning; A case study

A m i t r a z, a n i ns e c t i c i d e /a ca ri c i de of the f o r m a m i d i n e p e st i c i d e s group, is a ? 2 a d r e n e r g i c ag on i st a nd of t he a m i d i ne c h e m i ca l f a m il y generally us e d to c o n t r ol animal e c top a r a s i t e s. Poisoning due to am i t r a z i s r a r e and character...

متن کامل

Irradiated β-glucan enhances immune response to bacterial infection through CD4 and CD8 T-lymphocytes

Background: &beta-glucans are glucose polymers with a variety of stimulatory effects on the immune system. The objective of this study was to evaluate the immune-enhancing activities of low molecular weight gamma irradiated &beta-glucan (I&beta-g) extracted from Pleurotus ostreatus in response to Pseudomonas aeruginosa infection in rats. Materials and Methods: &beta-glucan (&beta-g) powder was ...

متن کامل

فراوانی اینتگرون‌های کلاس I و II در ایزوله‌های بالینی سودوموناس آئروژینوزا مولد متالوبتالاکتاماز

Background and Objective: Pseudomonas aeruginosa is an opportunistic nosocomial pathogen. Evidence suggests that the incidence of enzyme-producing strains of Pseudomonas aeruginosa Metalo Beta Lactamases (MBL) is a major problem in the treatment of infections caused by this organism. The aim of this study was to investigate the frequency of class I and II integrons among metalobetalactamase pro...

متن کامل

A New Indole Derivative Decreased SALL4 Gene Expression in Acute Promyelocytic Leukemia Cell Line (NB4)

Background: Acute myeloblastic leukemia (AML) is a clonal disorder due to bone marrow failure and uncontrolled proliferation of myeloid lineage. Acute promyelocytic leukemia (APL) is a subtype of AML. Heterocyclic compounds, such as indole, are considered as attractive candidates for cancer therapy, due to their abundance in nature and known biological activity. Sal-like protein (SALL4) is a zi...

متن کامل

Stability of $g$-Frame Expansions

In this paper we investigate the stability of one-sided perturbation to g-frame expansions. We show that if $Lambda$ is a g-frame of a Hilbert space $mathcal{H}$, $Lambda_{i}^{a}=Lambda_{i}+Theta_{i}$ where $Theta_{i} in mathcal{L}(mathcal{H},mathcal{H}_{i})$, and $widetilde{f}=sum_{i in J}Lambda_{i}^{star}widetilde{Lambda}_{i}^{a}f$, $widehat{f}=sum_{i in J}(Lambda_{i}^{a})^{star}widetilde{Lam...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2010