The Discovery and Development of Angiotensin II Antagonists

Carini, David J.; Christ, David D.; Duncia, John V.; Pierce, Michael E.

doi:10.1007/0-306-47384-4_3

Cited by 26 publications

(30 citation statements)

References 49 publications

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“…In 1982, Furukawa and coworkers discovered some benzylsubstituted imidazoles that were specific Ang-II antagonists [129]. These compounds served as leads to develop losartan [130], the first commercially available AT 1 antagonist, and valsartan [131] (structures 6 and 7) (Fig. 2).…”

Section: Ace Inhibitorsmentioning

confidence: 97%

Endogenous Vasoactive Peptides

Webb

Ksander²

2010

Burger's Medicinal Chemistry and Drug Discovery

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The control of vasomotor tone regulates the overall cardiovascular system and its responses to physiological and pathophysiological stress. It provides differential blood flow to regional vascular beds under normal physiologic conditions, at times of normal stress, such as exercise, and during conditions of pathological stress, such as congestive heart failure. Although the vascular system regulates many of its functions at the site of the blood vessel itself, other factors that may control vascular tone include the autonomic nervous system, circulating hormones functioning in an endocrine role, and reflex metabolic control. Many newly discovered peptides were found to be widespread in autonomic and sensory neurons innervating the vasculature, and they possess potent vasoactive effects on many blood vessels. Vasoactive peptides have been shown to play an important role in many pathological situations, for example, asthma, arthritis, vascular headaches, hypertension, and other cardiovascular diseases. In this chapter, we will outline the evidence for the different actions of various vasoactive peptides, their interaction with other systems, the possible role they have in diseases, and the present and future therapeutic use of vasoactive peptide agonists and antagonists.

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Section: Ace Inhibitorsmentioning

confidence: 97%

Endogenous Vasoactive Peptides

Webb

Ksander²

2010

Burger's Medicinal Chemistry and Drug Discovery

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“…LSR, the potassium salt of 2-n-butyl-4-chloro-5-hydroxymeth-yl-1-[(2%-(1H-tetra-zol-5-yl)biphenyl-4-yl)methyl]imidazole is a competitive nonpeptide angiotensin II antagonist, first marketed in 1995. It is recommended for treating hypertension [12] and hypertensive patients with diabetic nephropathy. It is available alone or in combination with other low dose thiazide diuretic to achieve an additive antihypertensive effect.…”

Section: Introductionmentioning

confidence: 99%

An Ultra-sensitive LC Method for the Simultaneous Determination of Paracetamol, Carbamazepine, Losartan and Ciprofloxacin in Bulk Drug, Pharmaceutical Formulation and Human Serum by Programming the Detector

Sultana¹,

Arayne²,

Ali³

2013

AJAC

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An ultra-sensitive LC method for the simultaneous quantitation of paracetamol, carbamazepine, losartan and ciprofloxacin have been developed and validated following the ICH guidelines at isobestic point and by programming the detector at individual wavelength of each component. −1 respectively. Percent recoveries > 98.37% from pharmaceutical formulation and human serum samples and RSD < 2% for inter-day and intra-day assay were obtained. The method was found to be robust and can be successfully applied for the determination of studied drugs in, pharmaceutical formulations and human serum without interference of excipients or endogenous components of serum.

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“…Losartan potassium is a highly specific, nonpeptide angiotensin II antagonist indicated for the treatment of hypertension [5]. It blocks the renin-angiotensin system by suppressing the effects of angiotensin II at its receptors [6], It is a weakly acidic yellowish white crystalline powder with a pK a of 4.9.…”

Section: Introductionmentioning

confidence: 99%