Chronic treatment with (W)DOI, a psychotomimetic 5-HT2 agonist, downregulates 5-HT2 receptors in rat brain
Abstract
(+/-)DOI (2,5-dimethoxy-4-iodo-phenylisopropylamine) is a hallucinogenic phenylalkylamine that has been characterized as a 5-HT2-selective agonist. Chronic treatment with (+/-)DOI [1.0 mg/kg/day (2.8 mumol/kg) for 8 days] significantly reduced the binding of [3H]ketanserin, [125I]LSD, and [125I]R-DOI as measured at single ligand concentrations in rat cortical homogenates. In saturation studies, chronic DOI treatment significantly lowered the Bmax of [3H]ketanserin binding and the high-affinity binding of [125I]R-DOI without altering the Kd values. In rats treated acutely with a single dose of (+/-)DOI, binding of [125I]R-DOI, [125I]LSD, and [3H]ketanserin was not significantly different from controls in membranes preincubated at 37 degrees C for 60 minutes. In all experiments nonspecific binding was determined by incubation with 1 microM ritanserin. This work demonstrates that chronic treatment with a 5-HT2-selective agonist hallucinogen reduces the number of binding sites for 5-HT2 agonists as well as for 5-HT2 antagonists.
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Saturation binding studies indicated chronic DOI treatment significantly lowered Bmax values for [3H]-ketanserin and R-[125I]-DOI without altering KD values.
“Saturation binding studies indicated that chronic DOI treatment significantly lowered the Bmax values for [3H]-ketanserin and R-[125I]-DOI (16) without altering the KD values.”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [80]
Chronic treatment with (+/−)-DOI (1 mg/kg daily for a week) significantly reduced binding of [3H]ketanserin, [125I]-LSD, and R-[125I]-DOI in rat cortical homogenates.
“Thus, chronic treatment with (+/−)-DOI (1 mg/kg daily for a week) significantly reduced the binding of [3H]ketanserin, [125I]-LSD (25), and R-[125I]-DOI (16) as measured at single ligand concentrations in rat cortical homogenates [80].”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [80]
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Strassman, R. J., Qualls, C. R., & Berg, L. M. (1996) · Biological Psychiatry · doi:10.1016/0006-3223(95)00200-6 · Cited by 130 · see citing works
Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans.
Cumming, P., Scheidegger, M., Dornbierer, D., Palner, M., Quednow, B. B., & Martin-Soelch, C. (2021) · Molecules · doi:10.3390/molecules26092451 · Cited by 43 · see citing works
- Authors
- MCKENNA, D.
- Affiliations
- National Institutes of Health (US)
- Corresponding author
- MCKENNA, D
- Venue
- Neuropsychopharmacology
- Publisher
- Elsevier BV
- Published
- 1989-03
- Volume
- 2
- Issue
- 1
- Pages
- 81-87
- ISSN
- 0893-133X (ISSN-L)
- OpenAlex
- W2018680292
- Cited by
- 86
- References
- 0
- Citations by year
- 2026: 1 · 2025: 2 · 2024: 1 · 2023: 2 · 2022: 3 · 2021: 1 · 2020: 1 · 2019: 2 · 2018: 2 · 2016: 1 · 2014: 1 · 2013: 1
- FWCI
- 6.67
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Neuropsychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- digital object identifiers, 5-HT2 receptor, ketanserin binding, receptor binding sites, receptor desensitization
- MeSH terms
- Amphetamines, Animals, Binding Sites, Cerebral Cortex, Humans, Male, Receptors, Serotonin, Down-Regulation, Rats
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