1. (a) There are two main types of adrenergic receptors: the a- and B-adrenoceptors. Noradrenaline shows slight selectivity for the a-adrenoceptor, whereas isoprenaline shows selectivity for the B-adrenoceptor. Adrenaline shows no selectivity and binds equally well to both the a- and B-adrenoceptors. Suggest an explanation for these differences in selectivity. OH OH OH Но, NH2 HO HO. Но Но HO Noradrenaline Isoprenaline Adrenaline (b) Isoprenaline undergoes metabolism to give the inactive metabolite shown below. Suggest why this metabolite does not bind to the B-adrenoceptor. OH H .N. Мео. но inactive metabolite of Isoprenaline

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1. (a) There are two main types of adrenergic receptors: the a- and B-adrenoceptors.
Noradrenaline shows slight selectivity for the a-adrenoceptor, whereas isoprenaline
shows selectivity for the B-adrenoceptor. Adrenaline shows no selectivity and
binds equally well to both the a- and B-adrenoceptors. Suggest an explanation for
these differences in selectivity.
OH
OH
OH
Но.
NH2
HO.
НО.
НО
Но
Но
Noradrenaline
Isoprenaline
Adrenaline
(b) Isoprenaline undergoes metabolism to give the inactive metabolite shown below.
Suggest why this metabolite does not bind to the B-adrenoceptor.
OH
MeO.
Но
inactive metabolite
of Isoprenaline
(c) R-Salbutamol is an anti-asthmatic agent that acts as an adrenergic agonist. Do you
think it is likely to show any selectivity between the a- and B-adrenoceptors?
Explain your answer.
OH
HOH2C,
Но
R-Salbutamol
Transcribed Image Text:1. (a) There are two main types of adrenergic receptors: the a- and B-adrenoceptors. Noradrenaline shows slight selectivity for the a-adrenoceptor, whereas isoprenaline shows selectivity for the B-adrenoceptor. Adrenaline shows no selectivity and binds equally well to both the a- and B-adrenoceptors. Suggest an explanation for these differences in selectivity. OH OH OH Но. NH2 HO. НО. НО Но Но Noradrenaline Isoprenaline Adrenaline (b) Isoprenaline undergoes metabolism to give the inactive metabolite shown below. Suggest why this metabolite does not bind to the B-adrenoceptor. OH MeO. Но inactive metabolite of Isoprenaline (c) R-Salbutamol is an anti-asthmatic agent that acts as an adrenergic agonist. Do you think it is likely to show any selectivity between the a- and B-adrenoceptors? Explain your answer. OH HOH2C, Но R-Salbutamol
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