Pharmacologically Active Substances of Mammalian Origin

Erspamer, V.

doi:10.1146/annurev.pa.01.040161.001135

Cited by 30 publications

(10 citation statements)

References 101 publications

(124 reference statements)

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“…Both groups of substances are of importance since it is possible that their effects are associated with the presence of structurally related compounds as chemical synaptic transmitters within the nervous system. Thus the indolylalkylamine 5-hydroxytryptamine and the catechol amines adrenaline noradrenaline and 3-hydroxytryptamine have been considered as transmitters although definite evidence is lacking (Erspamer, 1954(Erspamer, , 1961Brodie & Shore, 1957;Page, 1958;Costa, 1960;Carlsson, 1959;Rothballer, 1959).…”

mentioning

confidence: 99%

Pharmacological Studies Upon Neurones of the Lateral Geniculate Nucleus of the Cat

Curtis

Davis

1962

British Journal of Pharmacology and Chemotherapy

117

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Indoles related to 5-hydroxytryptamine, lysergic acid derivatives, phenethylamine derivatives and some other compounds have been applied electrophoretically to the neurones of the lateral geniculate nucleus of the cat anaesthetized with pentobarbitone sodium. Many of these compounds, particularly 4-, 5-and 7-hydroxytryptamine and ergometrine, depress the orthodromic excitation of the neurones by volleys in optic nerve fibres, but do not affect antidromic excitation by volleys in the optic radiation or chemical excitation by L-glutamic acid. It is concluded that the active depressants either block the access of the excitatory transmitter to subsynaptic receptors or prevent the release of the transmitter from optic nerve terminals. The structure-activity relationships of the depressant substances are discussed.Of recent years considerable interest has been maintained in a series of chemical compounds which have been classified as psychotomimetics since their administration produces clinical syndromes bearing some similarity to naturally occurring psychoses. These substances can be divided into two major groups. One contains an indole nucleus and includes substances such as (+)-lysergic acid diethylamide, certain of the ergot alkaloids, bufotenine, psilocybin and harmine. Members of the other group are related to the catechol amines and include adrenochrome and mescaline. Both groups of substances are of importance since it is possible that their effects are associated with the presence of structurally related compounds as chemical synaptic transmitters within the nervous system. Thus the indolylalkylamine 5-hydroxytryptamine and the catechol amines adrenaline noradrenaline and 3-hydroxytryptamine have been considered as transmitters although definite evidence is lacking (

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mentioning

confidence: 99%

Pharmacological Studies Upon Neurones of the Lateral Geniculate Nucleus of the Cat

Curtis

Davis

1962

British Journal of Pharmacology and Chemotherapy

117

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“…This disap pearance of pressor response was not caused by tachyphylaxis. There are considerable data on bio-active lipids (14,15). These data include hyper or hypo-tensive substances, some of which remain chemically undefined and other com pounds which although structurally defined have only low biological activities.…”

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confidence: 99%

Action of Depressor-I, a hypotensive phospholipid from bovine brain, on systemic and arterial blood pressures of various species.

et al. 1979

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Abstract-Effectsof "Depressor-I" (D-1), a new hypotensive phospholipid obtained from bovine brain lipid fraction, on systemic arterial blood pressure were investigated. The hypotensive activity of D-I in urethane anaesthetized rats was dose dependent and tachyphylaxis and/or sensitization were not observed. Increments of the respiration and the heart rate were observed with sharp falls in blood pressures following intra venous administration of D-1, in simultaneous recordings in anaesthetized rats. D-I elicited hypotension in all species of animals examined, and the sensitivities to D-I were much the same, however, there were two types in patterns of duration on responses and the durations were also dose dependent.D-I exhibited depressor-responses even in conscious rats, though responses were much smaller compared with those seen in anaesthetized rats. In a comparison of anaesthetic agents in rats, the highest hypo tensive activity of D-I was observed with pentobarbital anaesthesia, a moderate response was seen with a-chloralose and the least response was seen with urethane. In spinal rats or those pretreated with reserpine or antagonists, such as atropine, diphenhydra mine, propranolol and hexamethonium, D-I also elicited hypotension.These results suggest that "Depressor-I" does not elicit the depressor action via the stimulation of the central and the autonomic nervous systems but rather by a direct action on peripheral blood vessels.

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“…and a paracrine messenger from enterochromaffin (EC) cells (17) to initiate peristaltic and secretory reflexes (8,14,42,43,54). Released 5-HT must be inactivated to prevent its actions from becoming excessive and receptors from desensitizing.…”

Section: -Ht Is Utilized In the Bowel As A Neurotransmittermentioning

confidence: 99%

Expression and function of 5-HT₃receptors in the enteric neurons of mice lacking the serotonin transporter

Liu

Rayport

Jiang

et al. 2002

American Journal of Physiology-Gastrointestinal and Liver Physi

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. Expression and function of 5-HT 3 receptors in the enteric neurons of mice lacking the serotonin transporter. Am J Physiol Gastrointest Liver Physiol 283: G1398-G1411, 2002. First published September 4, 2002; 10.1152/ajpgi.00203.2002The actions of enteric 5-HT are terminated by 5-HT transporter (SERT)-mediated uptake, and gastrointestinal motility is abnormal in SERT Ϫ/Ϫ mice. We tested the hypothesis that adaptive changes in enteric 5-HT 3 receptors help SERT Ϫ/Ϫ mice survive despite inefficient 5-HT inactivation. Expression of mRNA encoding enteric 5-HT 3A subunits was similar in SERT ϩ/ϩ and Ϫ/Ϫ mice, but that of 5-HT3B subunits was fourfold less in SERT Ϫ/Ϫ mice. 5-HT3B mRNA was found, by in situ hybridization, in epithelial cells and enteric neurons. 5-HT evoked a fast inward current in myenteric neurons that was pharmacologically identified as 5-HT 3 mediated. The EC50 of the 5-HT response was lower in SERT ϩ/ϩ (18 M) than in SERT Ϫ/Ϫ (36 M) mice and desensitized rapidly in a greater proportion of SERT Ϫ/Ϫ neurons; however, peak amplitudes, steady-state current, and decay time constants were not different. Adaptive changes thus occur in the subunit composition of enteric 5-HT 3 receptors of SERT Ϫ/Ϫ mice that are reflected in 5-HT3 receptor affinity and desensitization. serotonin receptors; small intestine; enteric nervous system; electrophysiology 5-HT IS UTILIZED IN THE BOWEL as a neurotransmitter (24) and a paracrine messenger from enterochromaffin (EC) cells (17) to initiate peristaltic and secretory reflexes (8,14,42,43,54). Released 5-HT must be inactivated to prevent its actions from becoming excessive and receptors from desensitizing. To be inactivated, 5-HT must enter cells, because its catabolic enzymes are intracellular (25, 26). 5-HT is charged at physiological pH; therefore, its uptake across plasma membranes requires a high-affinity 5-HT transporter (5-HTT; SERT), which is identical in the brain (3, 4, 10), enteric nervous system (ENS), and gastrointestinal mucosa (11,12,65).Transgenic mice that lack SERT have been generated by deletion of the second exon by homologous recombination (1). High-affinity uptake of 5-HT is not detectable in either the brain (1) or the gut (12) of these animals. SERT Ϫ/Ϫ mice are viable into adulthood. In part, they survive because transporters other than SERT mediate 5-HT uptake (12, 58). In the gut, alternative transporters include the dopamine transporter and organic cation transporters-1 and -3 (12). The affinity of the dopamine transporter and the organic cation transporters for 5-HT is much lower than that of SERT; however, they have a high capacity and prevent 5-HT from accumulating to toxic levels. A number of presumably adaptive changes have been found in the brains of SERT Ϫ/Ϫ mice, including desensitization of presynaptic 5-HT 1A receptors (18,28,44) and a differential regulation of adenosine A 1 and A 2A receptors (50). The alternative transporters and other adaptive changes, however, compensate incompletely for the absence of SERT. Developmental def...

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Pharmacologically Active Substances of Mammalian Origin

Cited by 30 publications

References 101 publications

Pharmacological Studies Upon Neurones of the Lateral Geniculate Nucleus of the Cat

Pharmacological Studies Upon Neurones of the Lateral Geniculate Nucleus of the Cat

Action of Depressor-I, a hypotensive phospholipid from bovine brain, on systemic and arterial blood pressures of various species.

Expression and function of 5-HT₃receptors in the enteric neurons of mice lacking the serotonin transporter

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Pharmacologically Active Substances of Mammalian Origin

Cited by 30 publications

References 101 publications

Pharmacological Studies Upon Neurones of the Lateral Geniculate Nucleus of the Cat

Pharmacological Studies Upon Neurones of the Lateral Geniculate Nucleus of the Cat

Action of Depressor-I, a hypotensive phospholipid from bovine brain, on systemic and arterial blood pressures of various species.

Expression and function of 5-HT3receptors in the enteric neurons of mice lacking the serotonin transporter

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Expression and function of 5-HT₃receptors in the enteric neurons of mice lacking the serotonin transporter