Novel GABA analogues as hypotensive agents

Matheson, G.K.; Freed, Elisabeth H.; Tunnicliff, G.

doi:10.1016/0028-3908(86)90135-8

Cited by 15 publications

(6 citation statements)

References 20 publications

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“…Because of its structural relationship to γ-amino butyric acid (GABA), UCA has also been included in screening of in vivo biologic activity mediated by the GABA receptors, found typically in the central nervous system, and substantial effectiveness was observed (Matheson et al, 1986(Matheson et al, , 1987. Direct competition binding studies with UCA have been reported only on α 2 -and imidazol(in)e receptors 1 (no binding), and GABA (weak binding with trans-UCA; cis-isomer not studied) (Tunnicliff et al, 1985;Matheson et al, 1987).…”

Section: Urocanic Acid Binds To Gaba But Not To Histamine (H 1 H 2 mentioning

confidence: 99%

Urocanic Acid Binds to GABA but not to Histamine (H1, H2, or H3) Receptors

Laihia¹,

Jansén²,

Attila

et al. 1998

Journal of Investigative Dermatology

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Section: Urocanic Acid Binds To Gaba But Not To Histamine (H 1 H 2 mentioning

confidence: 99%

Urocanic Acid Binds to GABA but not to Histamine (H1, H2, or H3) Receptors

Laihia¹,

Jansén²,

Attila

et al. 1998

Journal of Investigative Dermatology

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“…A clinical trial conducted using a dietary supplement with a standardized content of monacolins demonstrated an 18% decrease in total cholesterol, a 23% decrease in lowdensity lipoprotein cholesterol, and a 15% decrease in triglycerides [13], which can help in alleviating arteriosclerosis [6]. GABA has several physiological functions, including neurotransmitting, hypotensive, and diuretic effects [19,26]. GABA is produced by the decarboxylation of glutamic acid by glutamate decarboxylase [21].…”

Section: Introductionmentioning

confidence: 99%

“…GABA is produced by the decarboxylation of glutamic acid by glutamate decarboxylase [21]. GABA, with two receptors-GABA A and GABA B , is the main suppressive nerve transmitter of the central nervous system [19]. Monascus has a prominent blood-pressurelowering effect, the antihypertensive substance being GABA [16,25].…”

Section: Introductionmentioning

confidence: 99%

Improvement of monacolin K, ?-aminobutyric acid and citrinin production ratio as a function of environmental conditions of Monascus purpureus NTU 601

Wang

Lee

Pan

2003

Journal of Industrial Microbiology and Biotechnology

131

107

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Monascus, a traditional Chinese fermentation fungus, is used as a natural dietary supplement. Its metabolic products monacolin K and gamma-aminobutyric acid (GABA) have each been proven to be a cholesterol-lowering drug and a hypotensive agent. Citrinin, another secondary metabolite, is toxic to humans, thus lowering the acceptability of red mold rice to the general public. In this study, the influence of different carbon and nitrogen sources, and fatty acid or oils, on the production of monacolin K, citrinin and GABA by Monascus purpureus NTU 601 was studied. When 0.5% ethanol was added to the culture medium, the production of citrinin decreased from 813 ppb to 561 ppb while monacolin K increased from 136 mg/kg to 383 mg/kg and GABA increased from 1,060 mg/kg to 7,453 mg/kg. In addition, response surface methodology was used to optimize culture conditions for monacolin K, citrinin and GABA production, and data were collected according to a three-factor (temperature, ethanol concentration and amount of water supplemented), three-level central composite design. When 500 g rice was used as a solid substrate with 120 ml water and 0.3% ethanol, the production of monacolin K at 30 degrees C increased from 136 mg/kg to 530 mg/kg, GABA production increased from 1,060 mg/kg to 5,004 mg/kg and citrinin decreased from 813 ppb to 460 ppb.

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“…It is well established that GABA plays an important role in cardiovascular regulation (5,9). Intracerebroventricular administration of GABA or its analogs induces a hypotensive effect (2,3,21). Conversely, intracerebroventricular injection of GABA antagonists or inhibitors of GABA synthesis increases blood pressure, heart rate, and sympathetic outflow (7,31,41,43).…”

mentioning

confidence: 99%

Reduced GABA inhibition of sympathetic function in renal-wrapped hypertensive rats

Martin

Haywood

1998

American Journal of Physiology-Regulatory, Integrative and Comp

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Animals with bilateral cannulas in the paraventricular nucleus were made hypertensive by a one-kidney, figure eight renal wrap procedure or sham operated. Femoral artery and vein catheters were inserted for arterial pressure measurement and plasma catecholamine determination. After recovery and 4 days after hypertension surgery, bicuculline methiodide or muscimol was microinjected into the paraventricular nucleus. In some rats, nitroprusside was infused intravenously to reflexly stimulate the sympathetic nervous system. In control rats, bicuculline increased blood pressure, heart rate, and plasma norepinephrine and epinephrine concentrations. In contrast, in hypertensive rats blood pressure did not change while the heart rate response was maintained. Plasma norepinephrine and epinephrine responses were reduced 75 and 68%, respectively. Muscimol injections decreased arterial pressure in the hypertensive rats. Heart rate responses to nitroprusside were similar in the two groups of rats, while the plasma catecholamine responses were attenuated in the hypertensive animals. These data suggest that GABA function in the paraventricular nucleus is reduced in renal wrap hypertension.

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Novel GABA analogues as hypotensive agents

Cited by 15 publications

References 20 publications

Urocanic Acid Binds to GABA but not to Histamine (H1, H2, or H3) Receptors

Urocanic Acid Binds to GABA but not to Histamine (H1, H2, or H3) Receptors

Improvement of monacolin K, ?-aminobutyric acid and citrinin production ratio as a function of environmental conditions of Monascus purpureus NTU 601

Reduced GABA inhibition of sympathetic function in renal-wrapped hypertensive rats

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