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5.4 The medical chemistry strategy

The strategy adopted was to start from first principles. Since prazosin is an alpha1 antagonist, it must compete with the agonist, noradrenaline, for the alpha1 receptor. So the Pfizer scientists decided to compare the structures of the two molecules and look for common structural features that might provide an insight into the way in which they bind to the receptor. One important observation was the fact that, at physiological pH, both compounds would be protonated, nor
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5.3 Project initiation

In the early 1970s a discovery was made independently by two different researchers, Klaus Starke in Germany and Salomon Langer in Argentina. Their results showed that there were two types of alpha receptor. The first type, which they called alpha1 is the one already described that is found on the blood vessel wall. The second type, which they called alpha2, is located on the nerve-ending itself. Noradrenaline binds to the alpha2 receptors when the alpha
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5.1 The medical background

Blood pressure is normally tightly controlled in the face of large variations in blood flow required by activities such as vigorous exercise. The diameter of the blood vessels is under the influence of the so-called sympathetic nervous system. Impulses from the brain stimulate the release of a chemical substance, noradrenaline (1), from the nerve-endings close to the vessel walls. The noradrenaline then diffuses to the blood vessel wall, where it interacts with a specific molecular sit
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2 Video activity

The video clip included in this section looks at the development of one particular drug. It examines the complex multidisciplinary process that was involved in its discovery. Before you watch the video, read through the Pre-viewing notes.


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1 The chemical industry

The chemical industry is one of the major contributors to the economies of advanced industrial nations.

The importance of organic chemistry in the pharmaceutical industry becomes apparent in the light of the fact that in the UK alone some £2.2b was spent in 1997 on research and development. Literally thousands of different compounds have to be synthesised and tested in the search for the one that will prove to be a successful and valuable therapeutic agent. As a result, the average cos
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Acknowledgements

Except for third party materials and otherwise stated (see terms and conditions), this content is made available under a Creative Commons Attribution-NonCommercial-ShareAlike 2.0 Licence

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2.1 Chemical periodicity

The chemistry of the elements is immensely varied. But amidst that variety there are patterns, and the best known and most useful is chemical periodicity: if the elements are laid out in order of atomic number, similar elements occur at regular intervals.

The discovery of chemical periodicity is particularly associated with the nineteenth-century Russian chemist Dmitri Ivanovich Mendeléev (Figure 16). The periodicity is represented graphically by Periodic Tables. Author(s): The Open University

2.3.1 Structural isomerism

In the saturated hydrocarbons, whose structural formulae are shown in Figure 16, it is not possible to form distinct isomers with just three or less carbon atoms linked together. There is only one way in which one carbon and four hydrogen atoms can be linked together, the single compound being methane, CH4. A simila
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1.2 Ethical examples

But is this a tenable position? In other words, is it only the people who use the technologies who carry the ethical burden? Conversely, is ethics of any interest to engineers, programmers and scientists? What, in the first place, constitutes an ethical issue? To begin examining these questions, let's look at some examples.

Example 1: Th
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Objectives for Section 3

After studying this section you should be able to do the following.

  • Recognise and use the terminology: disjoint union; power set (of a set); representation (of a data abstraction).

  • Use and interpret the notation:

     

    • X
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4.5 Vulnerability and rights

One of the assumptions that is made in order to justify social workers making such life-changing judgements is that some people are vulnerable and therefore need decisions made on their behalf. This assumption is not held by everyone and is often challenged by groups and individuals representing service users and by service users themselves.

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Testimonial - Vanessa Salvatore
http://graduatestudies.concordia.ca/gradproskills/ Testimony from Vanessa Salvatore, MA student in Creative Arts Therapies.
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Lesson 08 - One Minute Romanian
In lesson 8 of One Minute Romanian you will learn to count from one to ten. Remember - even a few phrases of a language can help you make friends and enjoy travel more. Find out more about One Minute Romanian at our website - http://www.oneminutelanguages.com. One Minute Romanian is brought to you by the Radio Lingua Network and is ©Copyright 2008.Author(s): No creator set

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Clemson awards first female in the nation Ph.D. in automotive engineering
CLEMSON — A Clemson University student is about to make national history as the first woman in the country to earn a Ph.D. in automotive engineering. Ala Qattawi is among nearly 200 students in Clemson's automotive engineering program who are pursuing graduate degrees in the male-dominated field. Qattawi's work involves concept cars and establishing a scientific approach for the design of structural origami in folded sheet metal. She said the technology will improve automobile efficiency and
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2.5 Intracellular receptors

Signal receptors are usually located at the cell surface. However, it is important to remember that there are some groups of receptors that do not fit into the general signal transduction model set out in Figure 2, These are intracellular receptors, which bind small or lipophilic molecules such as steroid hormones, which can cross the cell membrane. The signalling pathways activated by these receptors seem quite simple compared with the other pathways we shall be dealing with, but the same pr
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2.2 Receptor specificity

Binding of an extracellular signal to its receptor involves the same type of interactions as those between an enzyme and its substrate. Receptor specificity depends on the binding affinity between the ligand and the binding site on the receptor. The dissociation constant (KD) describes the affinity between receptors and their ligands.

Proteins can be thought of as consisting of various domains, and the different combinations of structural motifs in the extracellular re
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2.2.1 Using a calculator for scientific notation

You are likely to be doing many calculations with numbers in scientific notation, so it is important that you know how to input them on your calculator efficiently and how to interpret the results.

First, make sure that you can input numbers in scientific notation on your calculator. There are a couple of ways to do this, but the most straightforward is to use the special button provided for entering scientific notation. This might be labelled as EXP, EE, E or EX, but there is considera
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2.2 Going up: using scientific notation for large numbers

Think again about the value for the total volume of water stored on Earth: 1460 000 000 km3.

When dealing with large numbers such as one thousand four hundred and sixty million (1460 000 000), it is tedious to write the number in words or to keep writing all of those zeros. Worse still, it is very easy to lose some of the zeros or add extra ones by mistake. Fortunately, large numbers can be referred to without having to write out all of the zeros. The powers of ten not
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2.1 Where water occurs and how we measure it

When astronauts first ventured to the Moon in the late 1960s, they were captivated by a vision of the Earth in colour as it had never been seen before (Figure 2). It is not surprising that, after pictures like this were published, the Earth became known as the ‘blue planet’.

Figure 2
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