A 5-HT receptor-mediated interaction between 2,5-dimethoxy-4-methylamphetamine and citalopram in the rat

Eckler, J.R.; Reissig, Chad J.; Rabin, Richard A.; Winter, J.C.

doi:10.1016/j.pbb.2004.06.012

Cited by 10 publications

(7 citation statements)

References 31 publications

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“…[10] The (–)-DOM discriminative stimulus-potentiating effects of citalopram, furthermore, are attenuated by the highly selective 5-HT 2C antagonist, SB242084, [104,105] and mCPP, considered a selective, albeit poorly selective, 5-HT 2C agonist (relative to 5-HT 2A receptors), also potentiated the discriminative stimulus effects of (–)-DOM. [106] …”

Section: Receptor Systems Involved In the Htr Induced By Doimentioning

confidence: 99%

“…[10] The (À)-DOM discriminative stimulus-potentiating effects of citalopram, furthermore, are attenuated by the highly selective 5-HT 2C antagonist, SB242084, [104,105] and mCPP, considered a selective, albeit poorly selective, 5-HT 2C agonist (relative to 5-HT 2A receptors), also potentiated the discriminative stimulus effects of (À)-DOM. [106] Regarding the HTR in rats, direct frontal cortex injections of mCPP induced an HTR, an effect that was attenuated by systemic pretreatment with the selective 5-HT 2C receptor antagonist SDZ SER-082. [107] Interestingly, mCPP was more potent and produced more HTRs than DOI when injected centrally, [107] though its affinity and efficacy for stimulating 5-HT 2 receptors is substantially lower than DOI's.…”

Section: -Ht 2cmentioning

confidence: 99%

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Head‐twitch response in rodents induced by the hallucinogen 2,5‐dimethoxy‐4‐iodoamphetamine: a comprehensive history, a re‐evaluation of mechanisms, and its utility as a model

Canal

Morgan

2012

Drug Testing and Analysis

182

200

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Two primary animal models persist for assessing hallucinogenic potential of novel compounds and for examining the pharmacological and neurobiological substrates underlying the actions of classical hallucinogens, the two-lever drug discrimination procedure and the drug-induced head-twitch response (HTR) in rodents. The substituted amphetamine hallucinogen, serotonin 2 (5-HT2) receptor agonist, 2,5-dimethoxy-4-iodoamphetamine (DOI) has emerged as the most popular pharmacological tool used in HTR studies of hallucinogens. Synthesizing classic, recent, and relatively overlooked findings, addressing ostensibly conflicting observations, and considering contemporary theories in receptor and behavioural pharmacology, this review provides an up-to-date and comprehensive synopsis of DOI and the HTR model, from neural mechanisms to utility for understanding psychiatric diseases. Also presented is support for the argument that, although both the two-lever drug discrimination and the HTR models in rodents are useful for uncovering receptors, interacting proteins, intracellular signalling pathways, and neurochemical processes affected by DOI and related classical hallucinogens, results from both models suggest they are not reporting hallucinogenic experiences in animals.

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Section: Receptor Systems Involved In the Htr Induced By Doimentioning

confidence: 99%

Section: -Ht 2cmentioning

confidence: 99%

Head‐twitch response in rodents induced by the hallucinogen 2,5‐dimethoxy‐4‐iodoamphetamine: a comprehensive history, a re‐evaluation of mechanisms, and its utility as a model

Canal

Morgan

2012

Drug Testing and Analysis

182

200

View full text Add to dashboard Cite

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“…Using antagonist correlation analysis, Fiorella et al (1995a,b) concluded that the stimulus effects of LSD involved activation of 5-HT 2A receptors rather than 5-HT 2C receptors. Similarly, M100907, a selective 5HT 2A receptor antagonist, but not the 5HT 2C receptor antagonist SB 200,646, blocked the discriminative stimulus effects of phenethylamine hallucinogens (Schreiber et al, 1994;Eckler et al, 2004) Although 5-HT 2A receptors play a prominent role in mediating the stimulus effects of hallucinogenic drugs, the anatomical location of the relevant receptors is unclear. 5-HT 2A receptors are distributed throughout the brain, but are found in high density in various cortical regions (especially the frontal cortex), caudate nucleus, nucleus accumbens, olfactory nucleus, and claustrum (Pazos et al, 1985;Appel et al, 1990;López-Giménez et al, 1997).…”

Section: Introductionmentioning

confidence: 99%

Effects of clozapine and 2,5-dimethoxy-4-methylamphetamine [DOM] on 5-HT2A receptor expression in discrete brain areas

Doat-Meyerhoefer

Hard

Winter

et al. 2005

Pharmacology Biochemistry and Behavior

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Activation of 5-HT 2A receptors has been shown to be an essential component of the discriminative stimulus effects of indoleamine and phenethylamine hallucinogens. The objective of the present study was to determine the neuroanatomical location of the 5HT 2A receptors which may be responsible for the stimulus effects of the phenethylamine hallucinogen [−]2,5-dimethoxy-4-methylamphetamine (DOM). It was hypothesized that brain areas containing altered 5-HT 2A receptor expression in the context of a similar alteration in DOM-induced stimulus control might be important in mediating the stimulus effects of DOM. Fisher 344 rats were treated with either clozapine (25 mg/kg/day) or DOM (2 mg/kg/day) for 7 days, and the consequences of these drug treatment regimens on DOM-induced stimulus control and on 5-HT 2A receptor expression in several brain areas were determined. Chronic administration of clozapine was associated with a wide-spread decrease in levels of 5-HT 2A/2C receptors. Conversely, treatment with DOM had varied effects including a neuroanatomically selective decrease in 5-HT 2A/2C receptors levels that was restricted to the olfactory nucleus. Both chronic treatment with DOM and clozapine decreased the stimulus effects of DOM. The present findings suggest a role for the olfactory nucleus in producing the stimulus effects of DOM.

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“…Many 5-HT receptor agonists have activity at more than one receptor subtype; for example, 8-OH-DPAT induced hypothermia in rats is mediated by both 5-HT 1A and 5-HT 7 receptors (Hedlund et al, 2004). DOM has similar affinity for 5-HT 2A and 5-HT 2C receptors and reportedly exerts agonist activity at both receptor subtypes (Eckler et al, 2004; Fiorella et al, 1995; Li et al, 2009). …”

Section: Discussionmentioning

confidence: 99%

Effects of serotonin (5-HT)1A and 5-HT2A receptor agonists on schedule-controlled responding in rats: drug combination studies

Crocker

Koek

et al. 2010

Psychopharmacology

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Rationale Indirect acting serotonin (5-HT) receptor agonists (e.g., selective 5-HT reuptake inhibitors [SSRI]) stimulate multiple 5-HT receptors, although the role of particular receptors as well as interaction(s) among different receptors in the therapeutic effects of SSRIs is not fully understood. Objectives Relatively few studies have systematically examined direct-acting agonists in combination. This study examined the 5-HT1A receptor agonists 8-hydroxy-2-(di-n-propylamino tetralin hydrochloride (8-OH-DPAT; 0.01–10.0 mg/kg) and 3-chloro-4-fluorophenyl-4-fluoro-4-([(5-methyl-6-methylamino-pyridin-2-ylmethyl)-amino]-methyl)-piperidin-1-yl-methanone (F13714; 0.01–1.0 mg/kg) and the 5-HT2A receptor agonists 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM; 0.32–10.0 mg/kg) and dipropyltryptamine (DPT; 1.0–32.0 mg/kg), alone and in combination, in rats responding under a fixed ratio schedule of food presentation. Results When administered alone, each drug decreased the rate of responding in a dose-related manner with the potency order being F13714 > 8-OH-DPAT > DOM > DPT. WAY100635 (5-HT1A receptor antagonist; 0.01–0.1 mg/kg) attenuated the rate-decreasing effects of 8-OH-DPAT and F13714 while MDL100907 (5-HT2A receptor antagonist; 0.01–0.1 mg/kg) attenuated the rate-decreasing effects of DOM and DPT. Dose addition analysis showed that the interaction between 8-OH-DPAT and F13714, as well as the interaction between DOM and DPT, was additive. In contrast, the interaction between 8-OH-DPAT and DOM, as well as the interaction between F13714 and DOM, was infra-additive. Conclusions This study shows that, for some dose combinations, agonist actions at one 5-HT receptor subtype attenuate agonist actions at another 5-HT receptor subtype; thus, the combined neuropharmacological actions and therapeutic effects of indirect-acting agonists are not likely to be adequately characterized by examining in isolation activity at particular 5-HT receptor subtypes.

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A 5-HT receptor-mediated interaction between 2,5-dimethoxy-4-methylamphetamine and citalopram in the rat

Cited by 10 publications

References 31 publications

Head‐twitch response in rodents induced by the hallucinogen 2,5‐dimethoxy‐4‐iodoamphetamine: a comprehensive history, a re‐evaluation of mechanisms, and its utility as a model

Head‐twitch response in rodents induced by the hallucinogen 2,5‐dimethoxy‐4‐iodoamphetamine: a comprehensive history, a re‐evaluation of mechanisms, and its utility as a model

Effects of clozapine and 2,5-dimethoxy-4-methylamphetamine [DOM] on 5-HT2A receptor expression in discrete brain areas

Effects of serotonin (5-HT)1A and 5-HT2A receptor agonists on schedule-controlled responding in rats: drug combination studies

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