An approach to the design of brain-penetrating histaminergic agonists

RC Young, CR Ganellin, R Griffiths, RC Mitchell…

Index: Young; Ganellin; Griffiths; Mitchell; Parsons; Saunders; Sore European Journal of Medicinal Chemistry, 1993 , vol. 28, # 3 p. 201 - 211

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Citation Number: 31

Abstract

Abstract Known and novel histaminergic H 1-and H 2-receptor agonists were investigated as potentially potent and selective brain-penetrating compounds. Structural modifications were introduced in an attempt to favour passive diffusion across the blood-brain barrier by reducing hydrogen-bonding ability according to a previously developed model. While no novel compound was identified which satisfied our requirements for a brain-penetrating ...