A steric approach for the design of antihistamines with low muscarinic receptor antagonism

@article{Zhang2005ASA,
  title={A steric approach for the design of antihistamines with low muscarinic receptor antagonism},
  author={M. -Q. Zhang and Krzysztof Walczyński and Henk Timmerman},
  journal={Inflammation Research},
  year={2005},
  volume={44},
  pages={S90-S91}
}
For years, the clinical utility of histamine Hi-receptor antagonists (also known as antihistamines) has been hampered by two major side effects: (1) sedation, most likely resulting from blockade of histamine Hi-receptors in the central nervous system (CNS), and (2) muscarinic receptor antagonism, causing dry mouth, blurred vision, tachycardia and nervousness. The CNS depression of antihistamines can be avoided by designing drugs incapable of crossing the blood-brain barrier, e.g. by introducing… Expand
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The data presented here show that one of the newest antihistamines, desloratadine, and a first generation drug, diphenhydramine, are both competitive inhibitors of muscarinic receptor mediated slowing of the heart as measured using a Langendorff preparation. Expand

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