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A Potent Nonpeptide Antagonist of the Substance P (NK 1 ) Receptor
Abstract
CP-96,345 [(2 S , 3 S )- cis -2-(diphenylmethyl)- N -[(2-methoxyphenyl)-methyl]-1-azabicyclo[2.2.2]octan-3-amine] is a potent nonpeptide antagonist of the substance P (NK 1 ) receptor. CP-96,345 inhibited 3 H-labeled substance P binding and was a classical competitive antagonist in the NK 1 monoreceptor dog carotid artery preparation. CP-96,345 inhibited substance P-induced salivation in the rat, a classical in vivo bioassay, but did not inhibit NK 2 , NK 3 , or numerous other receptors; it is thus a selective NK 1 antagonist. This compound may prove to be a powerful tool for investigation of the physiological properties of substance P and exploration of its role in diseases.
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Yung-Chi, C., & Prusoff, W. H. (1973) · Biochemical Pharmacology · doi:10.1016/0006-2952(73)90196-2 · Cited by 12,922
Cited by
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Herrero, J. F., Laird, J. M. A., & Lopez-Garcia, J. A. (2000) · Progress in Neurobiology · doi:10.1016/s0301-0082(99)00051-9 · Cited by 714
Tachykinins in the gut. Part I. Expression, release and motor function
Holzer, P., & Holzer-Petsche, U. (1997) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(96)00195-7 · Cited by 310
Douglas, S. D., & Leeman, S. E. (2011) · Annals of the New York Academy of Sciences · doi:10.1111/j.1749-6632.2010.05826.x · Cited by 200
Neuropeptide receptor ligands as drugs for psychiatric diseases: the end of the beginning?
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Metadata
- Authors
- Snider, R. M., Constantine, J. W., Lowe, J. A., Longo, K. P., Lebel, W. S., Woody, H. A., Drozda, S. E., Desai, M. C., Vinick, F. J., Spencer, R. W., & Hess, H.-J.
- Venue
- Science
- Published
- 1991-01-25
- Volume
- 251
- Issue
- 4992
- Pages
- 435-437
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2031706219
- Cited by
- 859
- References
- 1
- FWCI
- 47.88
- Type
- journal article
- Language
- en
- Open access
- closed
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- The paper
- Snider, R. M., Constantine, J. W., Lowe, J. A., Longo, K. P., Lebel, W. S., Woody, H. A., Drozda, S. E., Desai, M. C., Vinick, F. J., Spencer, R. W., & Hess, H.-J. (1991). A Potent Nonpeptide Antagonist of the Substance P (NK 1 ) Receptor. Science. https://doi.org/10.1126/science.1703323
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
