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Development of a radioligand binding assay for 5‐HT4 receptors in guinea‐pig and rat brain
Open accessAbstract
The 5‐HT 4 receptor antagonist, GR113808, has been radiolabelled to a high specific activity with tritium. Characterization of specific [3 H]‐GR113808 binding in homogenates of guinea‐pig striatum and hippocampus revealed a single site of high affinity (Kd values 0.20 and 0.13 n m respectively). [3 H]‐GR113808 binding was reversible and displayed rapid kinetics such that association and dissociation were complete within 3 min. Specific [3 H]‐GR113808 binding was potently and stereoselectively inhibited by agonists and antagonists acting at the 5‐HT 4 receptor but not by compounds selective for other 5‐HT receptors or other neurotransmitter receptors. Autoradiographic analysis revealed a discrete localization in both guinea‐pig and rat brain with high concentrations of binding in brain areas such as the striatum, substantia nigra and olfactory tubercle. [3 H]‐GR113808 binding to homogenates of guinea‐pig striatum meets the criteria for labelling of the 5‐HT 4 receptor and, as such, represents the first characterization of this receptor in a radioligand binding assay.
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Cited by
Neuromodulatory transmitter systems in the cortex and their role in cortical plasticity
Gu, Q. (2002) · Neuroscience · doi:10.1016/s0306-4522(02)00026-x · Cited by 518
Receptors for 5-Hydroxytryptamine: Current perspectives on classification and nomenclature
Martin, G. R., & Humphrey, P. P. A. (1994) · Neuropharmacology · doi:10.1016/0028-3908(94)90058-2 · Cited by 305
Rochais, C., Lecoutey, C., Gaven, F., Giannoni, P., Hamidouche, K., Hedou, D., Dubost, E., Genest, D., Yahiaoui, S., Freret, T., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00115 · Cited by 129
Eglen, R. M., Bonhaus, D. W., Johnson, L. G., Leung, E., & Clark, R. D. (1995) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1995.tb16628.x · Cited by 102
Raffa, R. B., & Codd, E. E. (1996) · Life Sciences · doi:10.1016/0024-3205(96)00273-1 · Cited by 48
Metadata
- Authors
- Grossman, C. J., Kilpatrick, G. J., & Bunce, K. T.
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 1993-07
- Volume
- 109
- Issue
- 3
- Pages
- 618-624
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- OpenAlex
- W2053074524
- Cited by
- 289
- References
- 0
- FWCI
- 12.86
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Grossman, C. J., Kilpatrick, G. J., & Bunce, K. T. (1993). Development of a radioligand binding assay for 5‐HT4 receptors in guinea‐pig and rat brain. British Journal of Pharmacology. https://doi.org/10.1111/j.1476-5381.1993.tb13617.x
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