Potent agonist activity of DOB at 5-HT2 receptors in guinea pig trachea.
W A Heller, J M Baraban
European Journal of Pharmacology June 12, 1987 DOI: 10.1016/0014-2999(87)90345-1 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | In vitro pharmacology study Peer reviewed |
|---|---|
| Population | Guinea pig trachea tissue |
| Interventions | DOB 5-HT ketanserin pirenperone LY 53857 |
| Topics | Serotonin |
| Key points | DOB acted as a partial 5-HT agonist in guinea pig trachea with an EC50 of 25 nM, and its contractile response was blocked by the selective 5-HT2 antagonists ketanserin, pirenperone, and LY 53857, as was the response to 5-HT. The authors propose that DOB may be a useful agent for characterizing 5-HT2 receptor responses. |
Abstract
DOB, 4-bromo-2,5-dimethyloxyamphetamine, a potent hallucinogen, displays high affinity for the 5-HT2 receptor in binding assays. Since 5-HT contractile responses in guinea pig trachea are mediated by 5-HT2 receptors, we assessed the activity of DOB and related analogs in this preparation. DOB acts as a partial 5-HT agonist with an EC50 = 25 nM and is blocked by the potent selective 5-HT2 receptor antagonists ketanserin, pirenperone and LY 53857, as is 5-HT. These findings indicate that DOB may be a useful agent in characterizing 5-HT2 receptor responses.
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 3
- Dihydrobenzofuran Analogues of Hallucinogens. 4. Mescaline Derivatives Journal of Medicinal Chemistry September 1, 1997
- Analytical characterization of three hallucinogenic N-(2-methoxy)benzyl derivatives of the 2C-series of phenethylamine drugs. Drug Testing and Analysis August 1, 2013
- Differential interactions of dimethyltryptamine (DMT) with 5-HT1A and 5-HT2 receptors. Biochemical Pharmacology June 1, 1991