Discriminative stimulus properties of the serotonergic agent 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI).
Life Sciences September 1, 1986 DOI: 10.1016/0024-3205(86)90461-3 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Animal drug discrimination study Peer reviewed |
|---|---|
| Sample size | 6 |
| Population | Rats |
| Interventions | DOI DOM 8-OH DPAT TFMPP ketanserin |
| Dose | 0.5 mg/kg DOI (training dose); ED50 = 0.16 mg/kg DOI; ED50 = 0.49 mg/kg DOM |
| Topics | Serotonin |
| Key points | Rats trained to discriminate 0.5 mg/kg DOI from saline showed dose-related generalization (ED50 = 0.16 mg/kg), and the DOI cue generalized to the 5-HT2 agonist DOM (ED50 = 0.49 mg/kg) but not to 5-HT1A or 5-HT1B agonists, and was blocked by the 5-HT2 antagonist ketanserin. The authors suggest DOI's discriminative stimulus effects may be 5-HT2-mediated. |
Abstract
Using a two-lever drug discrimination procedure, six rats were trained to discriminate 0.5 mg/kg of racemic 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) from saline. Once trained, the animals demonstrated a dose-related decrease in discriminative performance upon administration of lower doses of DOI (ED50 = 0.16 mg/kg). DOI-stimulus generalization occurred with the putative 5-HT2 agonist DOM (ED50 = 0.49 mg/kg), but not with the 5-HT1A agonist 8-OH DPAT, or the 5-HT1B agonist TFMPP. Furthermore, the DOI stimulus could be antagonized by pretreatment of the animals with the 5-HT2 antagonist ketanserin. The present results, coupled with the prior demonstration that DOI possesses a significant affinity and selectivity for 5-HT2 binding sites, suggest that the discriminative stimulus effects of DOI may be 5-HT2-mediated.
Comparable studies
Other preclinical and animal studies on serotonin, most cited first.
| Study | Year | Design | Participants |
|---|---|---|---|
| Psilocybin induces rapid and persistent growth of dendritic spines in frontal cortex in vivo Mice | 2021 | Observational cohort | |
| Neurotoxicity of the psychedelic amphetamine, methylenedioxymethamphetamine. Rats (implied by typical neurochemical study context) | 1987 | Experimental study | |
| Psychedelics promote neuroplasticity through the activation of intracellular 5-HT2A receptors In vitro and in vivo (rodent) models | 2023 | Experimental study | |
| 3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Rat brain | 1987 | Animal experiment | |
| Comparison of the monoamine transporters from human and mouse in their sensitivities to psychostimulant drugs Human and mouse dopamine, norepinephrine, and serotonin transporters expressed in cells | 2006 | In vitro laboratory study |
Citations in the library
Cited by 17
- The hallucinogenic world of tryptamines: an updated review. Archives of Toxicology August 1, 2015
- DARK Classics in Chemical Neuroscience: NBOMes ACS Chemical Neuroscience October 28, 2019
- [125I]-2-(2,5-dimethoxy-4-iodophenyl)aminoethane ([125I]-2C-I) as a label for the 5-HT2 receptor in rat frontal cortex. Pharmacology, Biochemistry, and Behavior 1990
- Selective cross-tolerance to 5-HT1A and 5-HT2 receptor-mediated temperature and corticosterone responses. Pharmacology, Biochemistry, and Behavior August 1, 1989
- 1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (DOI): From an Obscure to Pivotal Member of the DOX Family of Serotonergic Psychedelic Agents - A Review. ACS Pharmacology & Translational Science June 14, 2024
and 12 more in the library
Cites 4
- Evidence for 5-HT2 involvement in the mechanism of action of hallucinogenic agents. Life Sciences December 17, 1984
- Mechanistic studies on DOM as a discriminative stimulus. Pharmacology, Biochemistry, and Behavior December 1985
- 5-HT1 and 5-HT2 binding properties of derivatives of the hallucinogen 1-(2,5-dimethoxyphenyl)-2-aminopropane (2,5-DMA). European Journal of Pharmacology June 15, 1984
- Antagonism of the effects of the hallucinogen DOM and the purported 5-HT agonist quipazine by 5-HT2 antagonists. European Journal of Pharmacology July 1, 1983