Research Summary on Vinpocetine

Vinpocetine's Effects on Na+ Channels and Neuroprotection: Studies indicate that vinpocetine is a potent blocker of voltage-gated Na+ channels, which may account for some of its pharmacological benefits. It effectively reduces [3H]batrachotoxin binding, Na+ currents, and offers protection against veratridine-induced cell death. Vinpocetine has also shown efficacy in reducing electric shock-induced seizures in mice.

Visualizing Microglial Activation: PET imaging with [((11))C]vinpocetine can visualize increased microglial activation following a stroke, indicating its utility in tracking inflammatory responses in the brain post-injury.

Vinpocetine's Protective Role: In brain cell cultures, vinpocetine can partially prevent excitotoxic cell death caused by glutamate, suggesting a direct protective effect on brain cells.

Enhancing Oral Bioavailability: The development of a self-microemulsifying drug delivery system (SMEDDS) for vinpocetine has improved its oral bioavailability by 1.72 times compared to commercial tablets.

Effects on Neurotransmitter Activity: Vinpocetine impacts neurotransmitter release in rat striatal nerve endings and could help modulate dopaminergic activity related to antiepileptic drugs' side effects.

Reduction of Glutamate Release: As a potential new antiepileptic drug, vinpocetine significantly reduces glutamate release at lower concentrations compared to other AEDs, suggesting benefits for epilepsy treatment.

Neuroprotective Effects of Vinpocetine: Research shows vinpocetine's neuroprotective effects in the context of glutamate toxicity, potentially targeting different pathways beyond neuronal peripheral-type benzodiazepine receptors.

Vinpocetine and Atherosclerosis: Vinpocetine demonstrates an anti-inflammatory role in atherosclerosis, reducing lesion formation and the uptake of oxidized LDL in macrophages.

Vinpocetine's Cognitive-Enhancing Effects: Animal studies indicate vinpocetine's potential in increasing the firing rate of noradrenergic neurons in the locus coeruleus, which may relate to its cognitive benefits.

Vasodilation Promotion: Vinpocetine may promote vasodilation by blocking calcium channels and selectively inhibiting CaM-PDE in vascular smooth muscle.

Direct CNS Effects: Clinical studies confirm vinpocetine's effectiveness in patients with organic psychosyndrome and ischemic stroke, improving blood flow and glucose utilization in the brain.

PBBS as a Disease Activity Marker: PBBS expression correlates with glial cell activation in diseased brain tissue, serving as a marker for brain disease activity and a potential target for PET imaging.

Antiepileptic Drug Comparison: Vinpocetine compared to other antiepileptic drugs reveals a greater effect on reducing neurotransmitter release, highlighting its potential as an anticonvulsant.

Peripheral Benzodiazepine Binding Sites: Vinpocetine acts as a potent ligand for PBBS, which may explain its pharmacological effects through the regulation of glial functions.

Antiepileptic Properties: Vinpocetine can inhibit convulsions and preserve hearing during epileptic events in guinea pigs.

ENOS in Cognitive Decline: The presence of eNOS in hippocampal pyramidal cells could relate to NO's role as a retrograde messenger in synaptic plasticity, possibly contributing to cognitive decline.

Effects on Blood Viscosity and Erythrocyte Deformability: Vinpocetine may influence blood circulation by affecting platelet aggregability and red blood cell flexibility.

Anti-inflammatory and Anti-cancer Potential: Vinpocetine has demonstrated anti-inflammatory effects by inhibiting NF-kappaB activation, and anti-cancer properties against breast cancer by promoting apoptosis and hindering cell migration.

Neuroprotective Effects in Dementia: Vinpocetine and its metabolite cAVA exhibit neuroprotective effects against neuronal damage and inflammation in a rat model of dementia.

References:

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2. Evolution of microglial activation in ischaemic core and peri-infarct regions after stroke: a PET study with the TSPO molecular imaging biomarker [((11))C]vinpocetine
3. Vinpocetin protects against excitotoxic cell death in primary cultures of rat cerebral cortex
4. NO/cGMP-dependent modulation of synaptic transmission
5. Preparation and evaluation of self-microemulsifying drug delivery system containing vinpocetine
6. Characterization of phenytoin, carbamazepine, vinpocetine and clorgyline simultaneous effects on sodium channels and catecholamine metabolism in rat striatal nerve endings
7. Effects of carbamazepine, phenytoin, valproic acid, oxcarbazepine, lamotrigine, topiramate and vinpocetine on the presynaptic Ca2+ channel-mediated release of [3H]glutamate: comparison with the Na+ channel-mediated release
8. Acute and chronic effects of vinpocetine on cerebral hemodynamics and neuropsychological performance in multi-infarct patients
9. Structural changes in the normally aging cerebral cortex of primates
10. Nitrate therapy: new aspects concerning molecular action and tolerance
11. Effects of Vinpocetine on mitochondrial function and neuroprotection in primary cortical neurons
12. Vinpocetine attenuates lipid accumulation and atherosclerosis formation
13. Noradrenergic and locus coeruleus modulation of the perforant path-evoked potential in rat dentate gyrus supports a role for the locus coeruleus in attentional and memorial processes
14. Effect of vinpocetine on noradrenergic neurons in rat locus coeruleus
15. Comparative effects of vinpocetine and 8-Br-cyclic GMP on the contraction and 45Ca-fluxes in the rabbit aorta
16. Role of sodium channel inhibition in neuroprotection: effect of vinpocetine
17. Ligands for peripheral benzodiazepine binding sites in glial cells
18. Vinpocetine inhibits glutamate release induced by the convulsive agent 4-aminopyridine more potently than several antiepileptic drugs
19. Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding
20. [Successful resuscitation from sudden death caused by Cavinton]
21. Restoration of neuronal plasticity by a phosphodiesterase type 1 inhibitor in a model of fetal alcohol exposure
22. Brain uptake and plasma metabolism of [11C]vinpocetine: a preliminary PET study in a cynomolgus monkey
23. Effects of isozyme-selective phosphodiesterase inhibitors on rat aorta and human platelets: smooth muscle tone, platelet aggregation and cAMP levels
24. [11C]vinpocetine: a prospective peripheral benzodiazepine receptor ligand for primate PET studies
25. Vinpocetine inhibits the epileptic cortical activity and auditory alterations induced by pentylenetetrazole in the guinea pig in vivo
26. Endothelial nitric oxide synthase localized to hippocampal pyramidal cells: implications for synaptic plasticity
27. Effects of TCV-3B (vinpocetine) on blood viscosity in ischemic cerebrovascular diseases
28. Characterization of vinpocetine effects on DA and DOPAC release in striatal isolated nerve endings
29. PET studies on the brain uptake and regional distribution of [11C]vinpocetine in human subjects
30. Resident vascular progenitor cells
31. Hypertension does not account for the accelerated atherosclerosis and development of aneurysms in male apolipoprotein e/endothelial nitric oxide synthase double knockout mice
32. Effect of RGH-2716 on learning and memory deficits of young and aged rats in water-labyrinth
33. Vinpocetine as a potent antiinflammatory agent
34. Amelioration of intracerebroventricular streptozotocin induced cognitive dysfunction and oxidative stress by vinpocetine -- a PDE1 inhibitor
35. The peripheral benzodiazepine receptor (Translocator protein 18kDa) in microglia: from pathology to imaging
36. Hematopoietic stem cells differentiate into vascular cells that participate in the pathogenesis of atherosclerosis
37. Idebenone and vinpocetine augment long-term potentiation in hippocampal slices in the guinea pig
38. Dopamine modulates the susceptibility of striatal neurons to 3-nitropropionic acid in the rat model of Huntington's disease
39. Luteolin, a non-selective competitive inhibitor of phosphodiesterases 1-5, displaced [3H]-rolipram from high-affinity rolipram binding sites and reversed xylazine/ketamine-induced anesthesia
40. [Cardiac toxicity of vincamine: a seven cases report of ventricular arrhythmias by parenteral administration of vincamine (author's transl)]
41. The neuroprotective drug vinpocetine prevents veratridine-induced [Na+]i and [Ca2+]i rise in synaptosomes
42. Vinpocetine increases cerebral blood flow and oxygenation in stroke patients: a near infrared spectroscopy and transcranial Doppler study
43. Effect of age on the pharmacokinetics of vinpocetine (Cavinton) and apovincaminic acid
44. Endogenous dopamine enhances the neurotoxicity of 3-nitropropionic acid in the striatum through the increase of mitochondrial respiratory inhibition and free radicals production
45. Age and gender effects on microglia and astrocyte numbers in brains of mice
46. Vinpocetine preferentially antagonizes quisqualate/AMPA receptor responses: evidence from release and ligand binding studies
47. Effects of vinpocetine on platelet aggregability and erythrocyte deformability
48. TSPO-specific ligand vinpocetine exerts a neuroprotective effect by suppressing microglial inflammation
49. Dissociation of coronary vascular tolerance and neurohormonal adjustments during long-term nitroglycerin therapy in patients with stable coronary artery disease
50. Monoamine oxidase: from genes to behavior
51. Regulation of translocator protein 18 kDa (TSPO) expression in health and disease states
52. Translocator protein 18 kDa (TSPO): molecular sensor of brain injury and repair
53. Proniosomes: a novel drug carrier preparation
54. Pharmacokinetics and metabolism of vincamine and related compounds
55. Vinpocetine enhances retrieval of a step-through passive avoidance response in rats
56. Redistribution of Na(V)1.8 in uninjured axons enables neuropathic pain
57. Cognitive effects of a Ginkgo biloba/vinpocetine compound in normal adults: systematic assessment of perception, attention and memory
58. Enhancement of low-threshold A-current of the neuronal membrane by vinpocetine
59. Inhibition of neuropathic pain by decreased expression of the tetrodotoxin-resistant sodium channel, NaV1.8
60. Age and disease related changes in the translocator protein (TSPO) system in the human brain: positron emission tomography measurements with [11C]vinpocetine
61. Effects of vinpocetine on cyclic nucleotide metabolism in vascular smooth muscle
62. Contact sensitivity to vincamine tartrate
63. Ethyl apovincaminate therapy in neurovascular diseases
64. Noradrenergic potentiation of excitatory transmitter action in cerebrocortical slices: evidence for mediation by an alpha 1 receptor-linked second messenger pathway
65. Requirement for generation of H2O2 for platelet-derived growth factor signal transduction
66. Norepinephrine exhibits two distinct profiles of action on sensory cortical neuron responses to excitatory synaptic stimuli
67. Glutamate neurotoxicity and diseases of the nervous system
68. The nootropic drug vinpocetine modulates different types of potassium currents in molluscan neurons
69. Vinpocetine and α-tocopherol prevent the increase in DA and oxidative stress induced by 3-NPA in striatum isolated nerve endings
70. Effects of several cerebroprotective drugs on NMDA channel function: evaluation using Xenopus oocytes and [3H]MK-801 binding
71. The synthesis of ethyl apovincaminate
72. Characterization of the participation of sodium channels on the rise in Na+ induced by 4-aminopyridine (4-AP) in synaptosomes
73. Translocator protein (18 kDa) TSPO: an emerging therapeutic target in neurotrauma
74. Vinpocetine prevents 4-aminopyridine-induced changes in the EEG, the auditory brainstem responses and hearing
75. Comparison of acute, chronic and post-treatment effects of carbamazepine and vinpocetine on hearing loss and seizures induced by 4-aminopyridine
76. Vinpocetine: nootropic effects on scopolamine-induced and hypoxia-induced retrieval deficits of a step-through passive avoidance response in rats
77. Selective suppression of the slow-inactivating potassium currents by nootropics in molluscan neurons
78. Omeprazole does not change the oral bioavailability or pharmacokinetics of vinpocetine in rats
79. Vinpocetine ameliorates acute hepatic damage caused by administration of carbon tetrachloride in rats
80. Mitochondrial apoptosis and the peripheral benzodiazepine receptor: a novel target for viral and pharmacological manipulation
81. Vinpocetine suppresses pathological vascular remodeling by inhibiting vascular smooth muscle cell proliferation and migration
82. [Human positron emission tomography with oral 11C-vinpocetine]
83. The use of Xenopus oocytes to evaluate drugs affecting brain Ca2+ channels: effects of bifemelane and several nootropic agents
84. Bioavailability of vinpocetine and interference of the time of application with food intake
85. Drug distribution in man: a positron emission tomography study after oral administration of the labelled neuroprotective drug vinpocetine
86. Vinpocetine attenuates the metabolic dysfunction induced by amyloid beta-peptides in PC12 cells
87. Upregulation of phosphodiesterase 1A1 expression is associated with the development of nitrate tolerance
88. Vinpocetine is a potent blocker of rat NaV1.8 tetrodotoxin-resistant sodium channels
89. Oxidized LDL, LOX-1 and atherosclerosis
90. Pharmacokinetics and comparative bioavailability of two vinpocetine tablet formulations in healthy volunteers by using the metabolite apovincaminic acid as pharmacokinetic parameter
91. Peripheral benzodiazepine receptors and mitochondrial function
92. Pharmacokinetics of vinpocetine in humans
93. Determination of apovincaminic acid in human plasma by high-performance liquid chromatography using solid-phase extraction and ultraviolet detection
94. Reversing brain damage in former NFL players: implications for traumatic brain injury and substance abuse rehabilitation
95. Psychopharmacological effects of vinpocetine in normal healthy volunteers
96. Dopamine uptake blockers nullify methamphetamine-induced decrease in dopamine uptake and plasma membrane potential in rat striatal synaptosomes
97. Optimized preparation of vinpocetine proliposomes by a novel method and in vivo evaluation of its pharmacokinetics in New Zealand rabbits
98. Pharmacokinetics of vinpocetine and its main metabolite apovincaminic acid before and after the chronic oral administration of vinpocetine to humans
99. In vitro-in vivo correlation of the pharmacokinetics of vinpocetine
100. Blockade of neuropathic pain by antisense targeting of tetrodotoxin-resistant sodium channels in sensory neurons
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102. [The role of vinpocetine in the treatment of cerebrovascular diseases based in human studies]
103. Vinpocetine inhibits NF-kappaB-dependent inflammation via an IKK-dependent but PDE-independent mechanism
104. Vinpocetine inhibits breast cancer cells growth in vitro and in vivo
105. Differential regulation of bovine brain calmodulin-dependent cyclic nucleotide phosphodiesterase isoenzymes by cyclic AMP-dependent protein kinase and calmodulin-dependent phosphatase
106. The effects of phosphodiesterase inhibition on cyclic GMP and cyclic AMP accumulation in the hippocampus of the rat
107. Effects of vinpocetine on the redistribution of cerebral blood flow and glucose metabolism in chronic ischemic stroke patients: a PET study
108. Effects of carbamazepine, phenytoin, lamotrigine, oxcarbazepine, topiramate and vinpocetine on Na+ channel-mediated release of [3H]glutamate in hippocampal nerve endings
109. Identification of inhibitory and calmodulin-binding domains of the PDE1A1 and PDE1A2 calmodulin-stimulated cyclic nucleotide phosphodiesterases
110. Effect of 4-aminopyridine on transmitter release in synaptosomes
111. Single and combined effects of carbamazepine and vinpocetine on depolarization-induced changes in Na+, Ca2+ and glutamate release in hippocampal isolated nerve endings
112. The role of peripheral benzodiazepine receptors (PBRs) in CNS pathophysiology
113. Clinical and non-clinical investigations using positron emission tomography, near infrared spectroscopy and transcranial Doppler methods on the neuroprotective drug vinpocetine: a summary of evidences
114. Nootropic agent vinpocetine blocks delayed rectified potassium currents more strongly than high-threshold calcium currents
115. Vinpocetine effects on cognitive impairments produced by flunitrazepam
116. Preparation, evaluation, and NMR characterization of vinpocetine microemulsion for transdermal delivery
117. Novel sugar esters proniosomes for transdermal delivery of vinpocetine: preclinical and clinical studies
118. Piracetam and vinpocetine ameliorate rotenone-induced Parkinsonism in rats
119. Vinpocetine protects from aminoglycoside antibiotic-induced hearing loss in guinea pig in vivo
120. Vinpocetine pharmacokinetics in elderly subjects
121. Peripheral benzodiazepine receptor: structure and function in health and disease
122. Protective activity of ethyl apovincaminate on ischaemic anoxia of the brain
123. Phosphodiesterase type 1 inhibition improves learning in rats exposed to alcohol during the third trimester equivalent of human gestation
124. Systemic exposure of vinpocetine in pregnant Sprague Dawley rats following repeated oral exposure: An investigation of fetal transfer
125. Neuroprotective effects of vinpocetine and its major metabolite cis-apovincaminic acid on NMDA-induced neurotoxicity in a rat entorhinal cortex lesion model
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127. Biochemical effects of ethyl apovincaminate
128. Vinpocetine selectively inhibits neurotransmitter release triggered by sodium channel activation
129. Role of vinpocetine in cerebrovascular diseases
130. Effects of selective inhibitors on cyclic nucleotide phosphodiesterases of rabbit aorta
131. 3-Nitropropionic acid's lethal triplet: cooperative pathways of neurodegeneration
132. Locus coeruleus activation facilitates memory encoding and induces hippocampal LTD that depends on beta-adrenergic receptor activation
133. Characterization of inhibitors of phosphodiesterase 1C on a human cellular system
134. Vinpocetine blockade of sodium channels inhibits the rise in sodium and calcium induced by 4-aminopyridine in synaptosomes
135. Visualising microglial activation in vivo
136. Protective effects of vinpocetine and structurally related drugs on the lethal consequences of hypoxia in mice
137. Enhanced oral bioavailability of vinpocetine through mechanochemical salt formation: physico-chemical characterization and in vivo studies
138. Vinpocetine attenuates lipid accumulation and atherosclerosis formation
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140. Memory Enhancers for Alzheimer's Dementia: Focus on cGMP
141. Vinpocetine Attenuates Pathological Cardiac Remodeling by Inhibiting Cardiac Hypertrophy and Fibrosis
142. Studies on Pharmacokinetic Drug Interaction Potential of Vinpocetine
143. Vinpocetine (A comprehensive profile)
144. Vinpocetine reduces carrageenan-induced inflammatory hyperalgesia in mice by inhibiting oxidative stress, cytokine production and NF-κB activation in the paw and spinal cord
145. Normobaric Hypoxia and Submaximal Exercise Effects on Running Memory and Mood State in Women
146. Effect of acute hypoxia on cognition: A systematic review and meta-regression analysis
147. Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation
148. Role of vinpocetine in ischemic stroke and poststroke outcomes: A critical review
149. Vinpocetine suppresses pathological vascular remodeling by inhibiting vascular smooth muscle cell proliferation and migration
150. Vinpocetine effects on cognitive impairments produced by flunitrazepam
151. Cognitive performance is associated with cerebral oxygenation and peripheral oxygen saturation, but not plasma catecholamines, during graded normobaric hypoxia
152. Vinpocetine enhances retrieval of a step-through passive avoidance response in rats
153. The influence of hypoxia and prolonged exercise on attentional performance at high and extreme altitudes: A pilot study
154. Vinpocetine regulates levels of circulating TLRs in Parkinson's disease patients
155. Psychopharmacological effects of vinpocetine in normal healthy volunteers
156. Vinpocetine: nootropic effects on scopolamine-induced and hypoxia-induced retrieval deficits of a step-through passive avoidance response in rats
157. Updates of Recent Vinpocetine Research in Treating Cardiovascular Diseases
158. Vinpocetine is the forthcoming adjuvant agent in the management of COVID-19
159. Asymptomatic ischemic cerebrovascular disorders and neuroprotection with vinpocetine
160. Vinpocetine Improves Scopolamine Induced Learning and Memory Dysfunction in C57 BL/6J Mice
161. [Investigation of the effect of vinpocetine on cerebral blood flow and cognitive functions]