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Chemical differentiation of histamine H1- and H2-receptor agonists
Abstract
Histamine exists predominantly as the NT-H tautomer of the monocation (IIa) at a physiological pH of 7.4 and structure-activity studies indicate that this tautomer is likely to be the pharmacologically active species for both H1 and H2 receptors. Effective H2-receptor agonists appear to require a prototropic tautomeric system whereas H1-receptor agonists do not need to be tautomeric. This identifies a chemical difference in the receptor requirements which provides the basis for obtaining selective histamine H1-receptor agonists. Thus 2-(2-aminoethyl)thiazole and 2-(2-aminoethyl)pyridine are nontautomeric and are highly selective agonists for histamine H1 receptors (H1:H2 ca. 90:1 and 30:1, respectively). In conjunction with the selective H2-receptor agonist, 4-methylhistamine, they are of great value for studying the pharmacology of histamine receptors.
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Cited by
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Barreiro, E. J., Kümmerle, A. E., & Fraga, C. A. M. (2011) · Chemical Reviews · doi:10.1021/cr200060g · Cited by 1,017
Buxton, I. L., Cheek, D. J., Eckman, D., Westfall, D. P., Sanders, K. M., & Keef, K. D. (1993) · Circulation Research · doi:10.1161/01.res.72.2.387 · Cited by 508
Imidazole- and imidazolium-containing polymers for biology and material science applications
Anderson, E. B., & Long, T. E. (2010) · Polymer · doi:10.1016/j.polymer.2010.02.006 · Cited by 407
Metadata
- Authors
- Durant, G. J., Ganellin, C. R., & Parsons, M. E.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1975-09
- Volume
- 18
- Issue
- 9
- Pages
- 905-909
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W1983510428
- Cited by
- 259
- References
- 0
- FWCI
- 5.18
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Chemical differentiation of histamine H1- and H2-receptor agonists. https://app.cochat.ai/papers/10.1021/jm00243a009
- The paper
- Durant, G. J., Ganellin, C. R., & Parsons, M. E. (1975). Chemical differentiation of histamine H1- and H2-receptor agonists. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm00243a009
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