(+)- And (−)-borneol: efficacious positive modulators of GABA action at human recombinant α1β2γ2L GABAA receptors

Granger, Renee E.; Campbell, Erica; Johnston, Graham A.R.

doi:10.1016/j.bcp.2005.01.002

Cited by 183 publications

(137 citation statements)

References 24 publications

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“…Os mecanismos que acarretam estes efeitos ainda não foram completamente elucidados, mas incluem antagonismo não-competitivo de receptores GABA A , responsáveis pela ação pró-convulsivante (Höld et al, 2000), e desensibilização de receptores 5-HT 3 (Deilm et al, 2004). Apesar da similaridade estrutural da tujona com o ∆ 1 -tetraidrocanabinol (∆ 1 -THC), a hipótese da ativação de receptores canabinóides CB 1 não foi demonstrada experimentalmente (Meschler & Howlett, 1999 (Granger et al, 2005).…”

Section: Linaloolunclassified

Terpenóides com atividade sobre o Sistema Nervoso Central (SNC)

Passos¹,

Arbo²,

Rates³

et al. 2009

Rev. bras. farmacogn.

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RESUMO:Os terpenóides constituem um vasto grupo de metabólitos secundários com ações sobre o SNC, destacando-se suas atividades sedativa, ansiolítica, antinociceptiva, anticonvulsivante, pró-convulsivante e alucinógena. Neste trabalho foi realizada uma revisão bibliográfica sobre terpenóides com ações descritas no SNC, enfocando moléculas e sistemas neurotransmissores relacionados com sua atividade. As substâncias abordadas encontram-se divididas em mono, sesqui, di, tri e meroterpenóides e incluem compostos isolados e plantas que apresentam ação principalmente sobre os sistemas neurotransmissores GABAérgico, glutamatérgico, dopaminérgico e opióide.Unitermos: Terpenóides, sistema nervoso central, neurotransmissores.ABSTRACT: "Terpenoids with activity in the Central Nervous System (CNS)". The terpenoids are a large group of secondary metabolites which display many activities in the CNS, such as sedative, ansiolytic, antinociceptive, anticonvulsant, pro-convulsant and hallucinogenic. In this work we performed a research on terpenoids that exert effects on the CNS, focusing molecules and neurotransmitter systems related to their actions. The substances approached were classified as mono, sesqui, di, tri and meroterpenoids and include isolated compounds and plants which exert activities mainly on GABAergic, glutamatergic, dopaminergic and opioid neurotransmitter systems.

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Section: Linaloolunclassified

Terpenóides com atividade sobre o Sistema Nervoso Central (SNC)

Passos¹,

Arbo²,

Rates³

et al. 2009

Rev. bras. farmacogn.

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“…Fa131 (trans-(2S,3R)-3-acetoxy-4′-methoxylavan, Figure 3) is a non-sedating anxiolytic and a selective positive modulator of α2-containing GABA A receptors, shown on the basis of eicacy [55,56]. The eicacy of 2100% enhancement exceeds the highest eicacy previously recorded, which was 1250% by (+)-borneol at these receptors [57].…”

Section: Synthetic Lavonoidsmentioning

confidence: 93%

Flavonoid Actions on Receptors for the Inhibitory Neurotransmitter GABA

Hinton¹,

Hanrahan²,

Johnston³

2017

Flavonoids - From Biosynthesis to Human Health

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Flavonoids, both naturally occurring and synthetic, are known to have multiple efects on the activation of ionotropic receptors for γ-aminobutyric acid (GABA), the major inhibitory neurotransmiter in our brains. They can act as positive or negative allosteric modulators, enhancing or reducing the efect of GABA. They can elicit a direct activation of the receptors. They can also act to modulate the action of other modulators. This ability to inluence function via their actions on GABA receptors permits a range of efects of lavonoids, including relief of anxiety, anticonvulsant, analgesic and sedative actions.

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“…Fragrant compounds may modulate mood through potentiation of the GABA A receptor response after being absorbed into the brain because hydrophobic compounds are easily absorbed through the blood-brain barrier in the same way as tranquilizers, sleeping drugs, and anesthetics. GABA A receptor channels are modulated not only by clinically important drugs such as benzodiazepines, barbiturates and various general anesthetics, but also by several compounds of plant origin including flavonoids, such as methyl-apigenin (Sheghart, 1995) or eogonin (Hui et al, 2002), polyacetylenes, (Baur et al, 2005), monoterpenes, such as borneol (Granger et al, 2005), and thymol (Garcia et al, 2006). Perez et al (1998) found neuropharmacological properties in the fruit of Solanum nigrum which possesses potential CNS-depressant action.…”

Section: Introductionmentioning

confidence: 99%

Potentiation of the Response of GABAA Receptors by Bangladeshi Medicinal Plants

Mubassara

Hossain

Ahmed

et al. 2009

FSTR

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As part of the search for new sources of mental health supplements, alcohol extracts of 11 Bangladeshi medicinal fruits and plants were investigated for neuropharmacological effects in mice and on ionotropic γ-aminobutyric acid receptors (GABA A receptors). The extracts of S. caseolaris, T. bellirica, S. cumini, and T. arjuna significantly potentiated the GABA-induced response of GABA A receptors expressed in Xenopus oocytes, though the extracts alone induced no response. In mice, administration of these extracts prolonged pentobarbital-induced sleeping time. Potentiation of GABA A receptor response reportedly generates anxiolytic, sedative, sleep-inducing and anesthetic activities in the human brain. Thus, these extracts may have potential regarding the development of a supplement with tranquilizing and sleepinducing effects that is beneficial for mental health.Keywords: Bangladeshi fruit, GABA A receptor, mangrove tree, pentobarbital-induced sleeping time, tranquilizer *To whom correspondence should be addressed. E-mail: aoshima@yamaguchi-u.ac.jp IntroductionAs society ages and the amount of lifestyle-related stress increases, there is increasing demand for the development of supplements which improve physical and mental health. Therefore, it is important to find new botanical resources for use as active ingredients for supplements or drugs.Over 1000 of the estimated 5000 species of phanerogams found in Bangladesh, Southeast Asia are regarded as having useful chemical constituents (Goni, 2003). A variety of these plants have been used traditionally as astringents, antiseptics, tonics, febrifuges and fish poison as they possess active compounds such as alkaloids, polyphenols, saponins, tanic acids, resins, waxes and fragrant compounds (Goni, 2003). However, despite the consumption and use of these herbs and fruits, little scientific data clarifying their physiological activities are available. There is some information available relating to their chemical constituents (Goni, 2003;Sadhu, et al., 2006) and biological properties (Scartezzini et al., 2005;Abdille et al., 2004; Lee et al., 2005). Our laboratory has recently reported the antioxidative, antiamylase, antiglucosidase and antihistamine release activities of some Bangladeshi fruits (Hossain et al., 2008).Various neurotransmitter receptors are involved in defining mental state, particularly the ionotropic γ-aminobutyric acid receptors (GABA A receptors), which are the main inhibitory neurotransmitter receptors in the human brain (Hossain et al., 2007). These heteropentamers composed of various α, β, γ, δ and ε subunits were found to be expressed in Xenopus laevis oocytes (Trauner et al., 2008). The potentiation of the response of these receptors by drugs such as benzodiazepine, pentobarbital and anesthetics induces tranquilizing, sleepinducing or anesthetic responses in humans (Nicholls, 1994;Chebib & Johnston, 2000;Harrison et al., 2000). It was found that fragrant compounds such as terpinen-4-ol, 1-octen-3-ol, and linalool potentiated the response of GAB...

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(+)- And (−)-borneol: efficacious positive modulators of GABA action at human recombinant α1β2γ2L GABAA receptors

Cited by 183 publications

References 24 publications

Terpenóides com atividade sobre o Sistema Nervoso Central (SNC)

Terpenóides com atividade sobre o Sistema Nervoso Central (SNC)

Flavonoid Actions on Receptors for the Inhibitory Neurotransmitter GABA

Potentiation of the Response of GABAA Receptors by Bangladeshi Medicinal Plants

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