Pharmacology, Biochemistry, and Behavior
January 2008
C M Krall, J B Richards, R A Rabin et al.
Based upon extensive studies in the rat, it has been suggested that stimulus control by LSD is mediated by 5-HT2A receptors, with serotonergic receptors of the 5-HT1A and 5-HT2C subtypes playing modulatory roles. In genetically modified mice lacking the serotonin transporter (SERT), 5-HT2A receptor density is decreased and, at a functional level, the head-twitch response following the...
Pharmacology, Biochemistry, and Behavior
January 2008
William E Fantegrossi, Chad J Reissig, Elyse B Katz et al.
N,N-dipropyltryptamine (DPT) is a synthetic tryptamine hallucinogen which has been used psychotherapeutically in humans, but has been studied preclinically only rarely. In the present studies, DPT was tested in a drug-elicited head-twitch assay in mice, and in rats trained to discriminate lysergic acid diethylamide (LSD), N,N-dimethyl-4-phosphoryloxytryptamine (psilocybin), or...
European Journal of Neuroscience
November 16, 2007
Susan Schenk, Lincoln S. Hely, Barbara Lake et al.
113 citations
Abstract 3,4‐Methylenedioxymethamphetamine (MDMA) self‐administration has been shown in animals with extensive drug histories, but only a small number of studies have examined high rates of responding maintained by MDMA in previously drug‐naïve animals. In the present study, influence of dose (0.25 or 1.0 mg/kg/infusion) on the acquisition of MDMA self‐administration was measured during daily...
Molecular Pharmacology
November 2007
Michael R Braden, David E Nichols
We assessed the relative importance of two serine residues located near the top of transmembrane helix 5 of the human 5-HT(2A) receptor, comparing the wild type with S5.43(239)A or S5.46(242)A mutations. Using the ergoline lysergic acid diethylamide (LSD), and a series of substituted tryptamine and phenethylamine 5-HT(2A) receptor agonists, we found that Ser5.43(239) is more critical for...
Journal of Neuroscience
October 24, 2007
Francis Rodriguez Bambico, Noam Katz, Guy Debonnel et al.
325 citations
Preclinical and clinical studies show that cannabis modulates mood and possesses antidepressant-like properties, mediated by the agonistic activity of cannabinoids on central CB1 receptors (CB1Rs). The action of CB1R agonists on the serotonin (5-HT) system, the major transmitter system involved in mood control and implicated in the mechanism of action of antidepressants, remains however poorly...
Proceedings of the National Academy of Sciences
October 9, 2007
Alexandra Jean, Grégory Conductier, Christine Manrique et al.
Anorexia nervosa is a growing concern in mental health, often inducing death. The potential neuronal deficits that may underlie abnormal inhibitions of food intake, however, remain largely unexplored. We hypothesized that anorexia may involve altered signaling events within the nucleus accumbens (NAc), a brain structure involved in reward. We show here that direct stimulation of serotonin...
Journal of Biological Chemistry
October 5, 2007
Miriam T Jacobs, Yuan-Wei Zhang, Scott D Campbell et al.
149 citations
Ibogaine, a hallucinogenic alkaloid with purported anti-addiction properties, inhibited serotonin transporter (SERT) noncompetitively by decreasing V(max) with little change in the K(m) for serotonin (5-HT). Ibogaine also inhibited binding to SERT of the cocaine analog 2beta-2-carbomethoxy-3-(4-[(125)I]iodophenyl)tropane. However, inhibition of binding was competitive, increasing the apparent...
Journal of Pharmacology and Experimental Therapeutics
October 2007
Ju Shi, Katerina J Damjanoska, Rakesh K Singh et al.
We previously demonstrated that 24-h treatment with (-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane HCl (DOI) causes phosphorylation of Galpha11 protein at serine 154 and that this phosphorylation causes desensitization of serotonin (5-HT) 2A receptor signaling in A1A1v cells (Shi et al., 2007). We now report that treatment of A1A1v cells with DOI for 24 h produces a greater reduction in the...
Pharmacology, Biochemistry, and Behavior
September 19, 2007
Chad J Reissig, Justin R Eckler, R A Rabin et al.
A previous investigation in our laboratory found that the stimulus effects of the 5-HT2A agonist, LSD, are potentiated by 5-HT1A receptor agonists including the prototypic agonist, 8-OH-DPAT. Also suggestive of behaviorally relevant interactions between 5-HT1A and 5-HT2A receptors are behavioral analyses of locomotor activity, head-twitch response, forepaw treading and production of the...
Australian & New Zealand Journal of Psychiatry
July 25, 2007
Edmund Silins, Jan Copeland, Paul Dillon
76 citations
Growth of the antidepressant market and widespread use of the illicit drug ecstasy (methylenedioxymethamphetamine; MDMA) creates a need to delineate the potential harms associated with the concomitant use of ecstasy and serotonergic pharmaceutical drugs. One such harm is serotonin syndrome. The study aimed to synthesize the risk of serotonin syndrome associated with the concomitant use of...