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Pharmacological characterization of 5-hydroxytryptamine4(5-HT4) receptors positively coupled to adenylate cyclase in adult guinea pig hippocampal membranes: effect of substituted benzamide derivatives.
Abstract
Adult guinea pig hippocampal membranes contain two 5-hydroxytryptamine (5-HT) receptors positively coupled with an adenylate cyclase. One is a typical 5-HT1A receptor and the second is a nonclassical 5-HT receptor that we previously proposed to call 5-HT4. Here, we show that 4-amino-5-chlor-2-methoxy-benzamide derivatives are agonists of 5-HT4 receptors in guinea pig hippocampal membranes. Their effects on the adenylate cyclase of these membranes are not additive with those of 5-HT but are additive with those of RU 24969, a typical 5-HT1 agonist. The effects of benzamides, as well as those of 5-HT, on 5-HT4 receptors are not blocked by 5-HT1, 5-HT2, or 5-HT3 antagonists except ICS 205 903, which does so with a low affinity (1 microM). The potency of benzamides (cisapride greater than BRL 24924 greater than zacopride greater than BRL 20627 greater than metoclopramide) is similar to their effect of 5-HT4 receptors positively coupled with an adenylate cyclase of fetal mouse colliculi neurons.
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Citations
Cited by
A review of central 5-HT receptors and their function
Barnes, N. M., & Sharp, T. (1999) · Neuropharmacology · doi:10.1016/s0028-3908(99)00010-6 · Cited by 3,161
Molecular biology of 5-HT receptors
Hannon, J., & Hoyer, D. (2008) · Behavioural Brain Research · doi:10.1016/j.bbr.2008.03.020 · Cited by 815
Molecular biology of 5-HT receptors
Boess, F. G., & Martin, I. L. (1994) · Neuropharmacology · doi:10.1016/0028-3908(94)90059-0 · Cited by 677
Multiplicity of mechanisms of serotonin receptor signal transduction
Raymond, J. R., Mukhin, Y. V., Gelasco, A., Turner, J., Collinsworth, G., Gettys, T. W., Grewal, J. S., & Garnovskaya, M. N. (2001) · Pharmacology & Therapeutics · doi:10.1016/s0163-7258(01)00169-3 · Cited by 466
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McCorvy, J. D., & Roth, B. L. (2015) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2015.01.009 · Cited by 372
Metadata
- Authors
- Bockaert, J., Sebben, M., & Dumuis, A.
- Venue
- Molecular Pharmacology
- Publisher
- Elsevier BV
- Published
- 1990-03
- Volume
- 37
- Issue
- 3
- Pages
- 408-411
- ISSN
- 0026-895X (ISSN-L)
- OpenAlex
- W2260556967
- Cited by
- 202
- References
- 0
- FWCI
- 6.48
- Type
- journal article
- Language
- en
- Open access
- closed
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- Bockaert, J., Sebben, M., & Dumuis, A. (1990). Pharmacological characterization of 5-hydroxytryptamine4(5-HT4) receptors positively coupled to adenylate cyclase in adult guinea pig hippocampal membranes: effect of substituted benzamide derivatives. Molecular Pharmacology. https://doi.org/10.1016/s0026-895x(25)10829-8
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