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Histamine and Obesity
The role of the histaminergic system in eating habits has been established in numerous animal and human studies. Histamine is best known as an allergic / inflammatory mediator; however, peripherally - produced histamine does not penetrate the blood-brain barrier (BBB) and its activities in the brain are independent of its peripheral actions. In the brain, histamine acts as a neurotransmitter and plays a major role in eating. Histamine activation of the post-synaptic H1 receptor decreases food consumption, an activity which can be mimicked by H1 agonists. In contrast, inhibition the H1 receptor results in increased food consumption and consequent weight gain. The pre-synaptic H3 receptor has an auto-regulatory role on histamine production. Thus, inhibition of the H3 receptor may also decrease food intake.
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Betahistine
Betahistine, an H1 receptor agonist and partial H3 receptor antagonist, is a generic prescription drug used on a worldwide basis, except in the US, to treat Ménière's disease (vertigo). With over 35 years of treatment in more than 100 million patients, betahistine has an excellent safety profile. Moreover, a post-marketing surveillance review, to be published in November 2006, Indicates that after more than 130 million patient exposures, only about 500 reports have been filed.
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Proof Of Concept (POC) Study in Humans
POC has already been achieved in two independently conducted preliminary clinical trials suggesting that the drug has potential for weight reduction in obese patients as well as for prevention of weight gain associated with anti-psychotic drug therapy.
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A double-blinded pilot study, evaluating administration of HistaleanTM versus placebo for 4 weeks in 20 obese women, showed a significant weight loss and reduced fat intake in the drug treated patients. The study was conducted by Dr. Nir Barak, Obecure's Chief Scientific Officer ("CSO") and a specialist in clinical nutrition and internal medicine at the Rabin Medical Center in Israel3.
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An open label study, evaluating the drug when administered in conjunction with olanzapine in 3 drug-naïve psychosis patients, showed that the drug prevented the weight gain normally associated with the anti-psychotic drug4.
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3. Barak, N. Clinical Interventions (2005) 209-P
4. Poyurovsky et. al., International Clinical Psychopharmacology (2005), 101-103.
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