Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures

Harada, Chie; Fujii, Yoko; Hirai, Tadashi; Shinomiya, Kazuaki; Kamei, Chiaki

doi:10.1016/j.brainresbull.2004.02.001

Cited by 12 publications

(5 citation statements)

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“…The electrodes were bipolar twisted stainless steel wires 200 μm in diameter. The electrode was connected to an implantable pulse generator unit (ISE1000SA, Unimec Co., Ltd., Japan), which was embedded in the skull with dental cement (15). Rats were continuously stimulated for 1 week after the implantation by implantable remote pulse generator system command equipment (ISE1010C, Unimec Co., Ltd.) and electronic stimulator (SEN-7203, Nihon Kohde, Japan).…”

Section: Methodsmentioning

confidence: 99%

Striatal Stimulation Nurtures Endogenous Neurogenesis and Angiogenesis in Chronic-Phase Ischemic Stroke Rats

et al. 2011

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Deep brain stimulation (DBS) is used to treat a variety of neurological disorders including Parkinson's disease. In this study, we explored the effects of striatal stimulation (SS) in a rat model of chronic-phase ischemic stroke. The stimulation electrode was implanted into the ischemic penumbra at 1 month after middle cerebral artery occlusion (MCAO) and thereafter continuously delivered SS over a period of 1 week. Rats were evaluated behaviorally coupled with neuroradiological assessment of the infarct volumes using magnetic resonance imaging (MRI) at pre- and post-SS. The rats with SS showed significant behavioral recovery in the spontaneous activity and limb placement test compared to those without SS. MRI visualized that SS also significantly reduced the infarct volumes compared to that at pre-SS or without SS. Immunohistochemical analyses revealed a robust neurogenic response in rats that received SS characterized by a stream of proliferating cells from the subventricular zone migrating to and subsequently differentiating into neurons in the ischemic penumbra, which exhibited a significant GDNF upregulation. In tandem with this SS-mediated neurogenesis, enhanced angiogenesis was also recognized as revealed by a significant increase in VEGF levels in the penumbra. These results provide evidence that SS affords neurorestoration at the chronic phase of stroke by stimulating endogenous neurogenesis and angiogenesis.

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Section: Methodsmentioning

confidence: 99%

Striatal Stimulation Nurtures Endogenous Neurogenesis and Angiogenesis in Chronic-Phase Ischemic Stroke Rats

et al. 2011

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“…[223][224][225] With respect to the anticonvulsive effects of H 3 R antagonists various studies report the beneficial use in distinct seizure models, e.g. electrically induced convulsions, 227,228) kindling, 229,230) and pentylenetetrazole-(PTZ) induced seizures. 231) From additional studies in mice it is deduced that combinatory application of selective H 3 R antagonists and common antiepileptic drugs (AEDs) could provide protection against maximal electroshock-(MES) and PTZ-induced seizures.…”

Section: )mentioning

confidence: 99%

Histamine H3 Receptor Antagonists Go to Clinics

Sander

Kottke

Stark

2008

Biological & Pharmaceutical Bulletin

185

118

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INTRODUCTIONThe biogenic amine histamine, 2-(1H-imidazol-4-yl)-ethanamine, is produced by decarboxylation of L-histidine and is implicated in a wide range of physiological and pathophysiological functions. It is metabolised by histamine N tmethyltransferase (HMT) and mono-or diaminoxidase. Histamine is mainly acting via four distinct metabotropic histamine receptor subtypes (H 1 R-H 4 R), which have meanwhile all been cloned. Whereas antagonists for H 1 R and H 2 R subtypes have been blockbusters in therapy of allergy and ulcer, respectively, antagonists for H 3 R and H 4 R subtypes are not on the market. The recently described H 4 R seems to be involved in inflammatory and immunomodulatory processes. H 3 Rs play a central role in neurotransmission of histamine and in control of many other neurotransmitters. Several antagonists are in preclinical and some in clinical stage of development. PHARMACOLOGICAL BACKGROUND Auto-and HeteroreceptorThe H 3 R was first described in 1983 as a presynaptic autoreceptor, which mediates synthesis of histamine and inhibition of its release from histaminergic neurons in slices of rat cerebral cortex. 1) Localisation studies in rodents show a predominance in distinct regions of the central nervous system (CNS) as the H 3 R is mainly located in cerebral cortex, hippocampus, amygdala, nucleus accumbens, globus pallidus, striatum, and hypothalamus 2-5) ( Fig. 1). In addition, it is expressed in the peripheral nervous system, e.g. in gastrointestinal tract, airways and cardiovascular system. 6) Molecular aspects of the receptor, [7][8][9][10] structure-activity relationships (SAR) of ligands, [11][12][13][14][15][16][17][18][19] and pharmacology [20][21][22][23][24][25][26] have recently been resumed in many excellent reviews. This contribution focuses on the development of clinical candidates and the multifaceted potential indications targeted.In mammalian brain histaminergic neurons originate in the tuberomammillary nucleus (TMN) spreading into above mentioned brain regions, where they control histamine levels by regulation of synthesis and liberation rates 27) and modulate different neuronal systems. 28) H 3 R expression is not solely restricted to histaminergic neurons: due to its function as a heteroreceptor it can be found on colocalised neurons, and H 3 R activation modulates the release of various important neurotransmitters, i.e. dopamine, [29][30][31][32][33] acetylcholine, [34][35][36][37] norepinephrine, 38,39) serotonin, 40,41) GABA, [42][43][44] glutamate, 45) and substance P. [46][47][48] Therefore, histaminergic neurons and the cross-linkage between major neurotransmitter systems are involved in many (patho)physiological brain functions, including vigilance, memory processes, feeding behaviour and locomotor activity (Fig. 2). Interneuron cross-talk and adaptive processes seem to be important factors in H 3 Rmediated signalling. Molecular AspectsThe human histamine H 3 receptor (hH 3 R) cDNA firstly described 1999 encodes a 445 amino acid protein and belongs to the his...

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“…Prolonged release of histamine in response to brain ischaemic insults and alleviation of neuronal damage upon post‐ischaemic histamine administration suggests it has a neuroprotective role (reviewed by Adachi, 2005). Histaminergic drugs, most importantly H 3 receptor antagonists or inverse agonists, which are considered to be a class of perspective drugs for the treatment of diverse neurological and neuropsychiatric disorders (reviewed by Leurs et al ., 2011; Passani and Blandina, 2011), in view of the findings from various basic experimental models of epilepsy in rodents, are envisaged to possess promising anticonvulsive properties (Vohora et al ., 2000; 2001; 2010; Harada et al ., 2004a,b).…”

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confidence: 99%

Histamine H₃receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives

Bhowmik

Khanam

Vohora

2012

British J Pharmacology

105

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The central histaminergic actions are mediated by H1, H2, H3 and H4 receptors. The histamine H3 receptor regulates the release of histamine and a number of other neurotransmitters and thereby plays a role in cognitive and homeostatic processes. Elevated histamine levels suppress seizure activities and appear to confer neuroprotection. The H3 receptors have a number of enigmatic features like constitutive activity, interspecies variation, distinct ligand binding affinities and differential distribution of prototypic splice variants in the CNS. Furthermore, this Gi/Go‐protein‐coupled receptor modulates several intracellular signalling pathways whose involvement in epilepsy and neurotoxicity are yet to be ascertained and hence represent an attractive target in the search for new anti‐epileptogenic drugs. So far, H3 receptor antagonists/inverse agonists have garnered a great deal of interest in view of their promising therapeutic properties in various CNS disorders including epilepsy and related neurotoxicity. However, a number of experiments have yielded opposing effects. This article reviews recent works that have provided evidence for diverse mechanisms of antiepileptic and neuroprotective effects that were observed in various experimental models both in vitro and in vivo. The likely reasons for the apparent disparities arising from the literature are also discussed with the aim of establishing a more reliable basis for the future use of H3 receptor antagonists, thus improving their utility in epilepsy and associated neurotoxicity.

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Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures

Cited by 12 publications

References 12 publications

Striatal Stimulation Nurtures Endogenous Neurogenesis and Angiogenesis in Chronic-Phase Ischemic Stroke Rats

Striatal Stimulation Nurtures Endogenous Neurogenesis and Angiogenesis in Chronic-Phase Ischemic Stroke Rats

Histamine H3 Receptor Antagonists Go to Clinics

Histamine H₃receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives

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Inhibitory effect of iodophenpropit, a selective histamine H3 antagonist, on amygdaloid kindled seizures

Cited by 12 publications

References 12 publications

Striatal Stimulation Nurtures Endogenous Neurogenesis and Angiogenesis in Chronic-Phase Ischemic Stroke Rats

Striatal Stimulation Nurtures Endogenous Neurogenesis and Angiogenesis in Chronic-Phase Ischemic Stroke Rats

Histamine H3 Receptor Antagonists Go to Clinics

Histamine H3receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives

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Histamine H₃receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives