Effects of para-methoxyamphetamine and 2,5-dimethoxyamphetamine on serotonergic mechanisms. 1978

L F Tseng

A comparison of serotonergic effects of (+/-)-para-methoxyamphetamine (PMA) and (+/-)-2,5-dimethoxyamphetamine (2,5-DMA) was studied in rats. The activation of myoclonic twitch activity (MTA) of suprahyoideal muscle in urethane-anesthetized rats has been reported previously to involve central serotonergic and dopaminergic mechanisms. PMA (0.1--3.2 mg/kg i.v.) and 2,5-DMA (2--16 mg/kg i.v.) increased the MTA. The increased MTA caused by both PMA and 2,5-DMA was blocked by a 5-HT receptor blocker, methysergide, indicating that a serotonergic mechanism was involved. The increased MTA induced by PMA was reduced by a 5-HT synthesis inhibitor, para-chlorphenylalanine, (pCPA), and by a 5-HT uptake inhibitor, chlorimipramine. On the other hand, the increased MTA induced by 2,5-DMA was not blocked by pCPA or chlorimipramine. Using a ventricular perfusion technique in urethane-anesthetized rats, PMA (1.6 mg/kg) effectively increased the release of 3H-radioactivity from brain preloaded with 3H-5-HT before the initiation of perfusion whereas 2,5-DMA (16 mg/kg) decreased the release of 3H-radioactivity. Analysis of the perfusate by thin layer chromatography for 3H-5-HT and 3H-5-HIAA revealed an increased release of unchanged 3H-5-HT in the perfusate after the injection of PMA. The ratio of 3H-5-HT to 3H-5-HIAA was markedly increased after PMA but no alteration of this ratio was observed after 2,5-DMA. It is concluded that PMA elicits its pharmacological action indirectly by releasing 5-HT while 2,5-DMA acts directly on 5-HT receptors.

UI MeSH Term Description Entries
D007276 Injections, Intraventricular Injections into the cerebral ventricles. Intraventricular Injections,Injection, Intraventricular,Intraventricular Injection
D008297 Male Males
D009119 Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D004290 DOM 2,5-Dimethoxy-4-Methylamphetamine A psychedelic phenyl isopropylamine derivative, commonly called DOM, whose mood-altering effects and mechanism of action may be similar to those of LSD. 2,5-Dimethoxy-4-Methylamphetamine,2,5-Dimethoxy-4-Methylamphetamine (DOM),1-(2,5-Dimethoxy-4-Methylphenyl)-2-Aminopropane,2 5 DOM,2,5-Dimethoxy-4-Methylamphetamine Hydrochloride, (+,-)-Isomer,2,5-Dimethoxy-4-Methylamphetamine Hydrochloride, (R)-Isomer,2,5-Dimethoxy-4-Methylamphetamine Hydrochloride, (S)-Isomer,2,5-Dimethoxy-4-Methylamphetamine, (+,-)-Isomer,2,5-Dimethoxy-4-Methylamphetamine, (R)-Isomer,2,5-Dimethoxy-4-Methylamphetamine, (S)-Isomer,2,5-Dimethoxy-4-Methylamphetamine, Hydrochloride,2,5 Dimethoxy 4 Methylamphetamine,2,5-Dimethoxy-4-Methylamphetamine, DOM,DOM 2,5 Dimethoxy 4 Methylamphetamine
D000662 Amphetamines Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012701 Serotonin A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator. 5-HT,5-Hydroxytryptamine,3-(2-Aminoethyl)-1H-indol-5-ol,Enteramine,Hippophaine,Hydroxytryptamine,5 Hydroxytryptamine
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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