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Blarcamesine
Blarcamesine (developmental code name ANAVEX 2-73) is an experimental drug which is under development for the treatment of Alzheimer's disease and a variety of other indications. Blarcamesine acts as an agonist of the sigma σ1 receptor, the muscarinic acetylcholine M1 receptor, and the ionotropic glutamate NMDA receptor. The drug was developed by Anavex Life Sciences. As of August 2024, it is in preregistration for Alzheimer's disease, phase 2/ 3 clinical trials for fragile X syndrome and Rett syndrome, phase 2 trials for Parkinson's disease, and phase 1 trials for Angelman syndrome and infantile spasms. It was also under development for the treatment of amyotrophic lateral sclerosis (ALS), anxiety disorders, autistic spectrum disorders, cognition disorders, multiple sclerosis, and stroke, but development for these indications was discontinued. Pharmacology Pharmacodynamics Blacarmesine acts primarily as an agonist of the sigma σ1 receptor (affinity () = 860nM). T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma-1 Receptor
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a Chaperone (protein), chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the ''SIGMAR1'' gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system. It has been implicated in several phenomena, including cardiovascular function, schizophrenia, clinical depression, the effects of cocaine abuse, bipolar disorder, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand (biochemistry), ligand for the σ1 receptor has yet to be conclusively identified, but tryptaminergic trace amines and neuroactive steroids have been found to activate the receptor. Especially progesterone, but also testosterone, pregnenolone sulfate, N,N-dimethy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Drug
An experimental drug is a medicinal product (a drug or vaccine) that has not yet received drug approval, approval from governmental regulatory agency, regulatory authorities for routine use in human medicine, human or veterinary medicine. A medicinal product may be approved for use in one disease or condition but still be considered experimental for other diseases or conditions. United States In the United States, the body responsible for approval is the Food and Drug Administration (FDA), which must grant the substance Investigational New Drug (IND) status before it can be tested in human clinical trials. IND status requires the drug's sponsor to submit an IND application that includes data from laboratory and animal testing for drug safety, safety and efficacy. A drug that is made from a living organism or its products undergoes the same approval process but is called a biologics license application (BLA). Biological drugs include antibodies, interleukins, and vaccines. In 2018 f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amyotrophic Lateral Sclerosis
Amyotrophic lateral sclerosis (ALS), also known as motor neuron disease (MND) or—in the United States—Lou Gehrig's disease (LGD), is a rare, Terminal illness, terminal neurodegenerative disease, neurodegenerative disorder that results in the progressive loss of both upper and lower motor neurons that normally control Skeletal muscle, voluntary muscle contraction. ALS is the most common form of the motor neuron diseases. ALS often presents in its early stages with gradual muscle Spasticity, stiffness, Fasciculation, twitches, Muscle weakness, weakness, and Muscle atrophy, wasting. Motor neuron loss typically continues until the abilities to eat, speak, move, and, lastly, breathe are all lost. While only 15% of people with ALS also fully develop frontotemporal dementia, an estimated 50% face at least some minor difficulties with cognitive disorder, thinking and behavior. Depending on which of the aforementioned symptoms develops first, ALS is classified as ''limb-onset'' (b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
β-amyloid
Amyloid beta (Aβ, Abeta or beta-amyloid) denotes peptides of 36–43 amino acids that are the main component of the amyloid plaques found in the brains of people with Alzheimer's disease. The peptides derive from the amyloid-beta precursor protein (APP), which is cleaved by beta secretase and gamma secretase to yield Aβ in a cholesterol-dependent process and substrate presentation. Both neurons and oligodendrocytes produce and release Aβ in the brain, contributing to formation of amyloid plaques. Aβ molecules can aggregate to form flexible soluble oligomers which may exist in several forms. It is now believed that certain misfolded oligomers (known as "seeds") can induce other Aβ molecules to also take the misfolded oligomeric form, leading to a chain reaction akin to a prion infection. The oligomers are toxic to nerve cells. The other protein implicated in Alzheimer's disease, tau protein, also forms such prion-like misfolded oligomers, and there is some evidence that misfo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Long-term Memory
Long-term memory (LTM) is the stage of the Atkinson–Shiffrin memory model in which informative knowledge is held indefinitely. It is defined in contrast to sensory memory, the initial stage, and short-term or working memory, the second stage, which persists for about 18 to 30 seconds. LTM is grouped into two categories known as explicit memory (declarative memory) and implicit memory (non-declarative memory). Explicit memory is broken down into episodic and semantic memory, while implicit memory includes procedural memory and emotional conditioning. Stores The idea of separate memories for short- and long-term storage originated in the 19th century. One model of memory developed in the 1960s assumed that all memories are formed in one store and transfer to another store after a small period of time. This model is referred to as the "modal model", most famously detailed by Shiffrin. The model states that memory is first stored in sensory memory, which has a large capacit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Short-term Memory
Short-term memory (or "primary" or "active memory") is the capacity for holding a small amount of information in an active, readily available state for a short interval. For example, short-term memory holds a phone number that has just been recited. The duration of short-term memory (absent rehearsal or active maintenance) is estimated to be on the order of seconds. The commonly cited capacity of 7 items, found in Miller's Law, has been superseded by 4±1 items. In contrast, long-term memory holds information indefinitely. Short-term memory is not the same as working memory, which refers to structures and processes used for temporarily storing and manipulating information. Stores The idea of separate memories for short-term and long-term storage originated in the 19th century. A model of memory developed in the 1960s assumed that all memories are formed in one store and transfer to other stores after a small period of time. This model is referred to as the "modal model", mo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Competitive Inhibition
Competitive inhibition is interruption of a chemistry, chemical pathway owing to one chemical substance inhibiting the effect of another by competing with it for molecular binding, binding or chemical bond, bonding. Any metabolism, metabolic or chemical messenger (other), chemical messenger system can potentially be affected by this principle, but several classes of competitive inhibition are especially important in biochemistry and medicine, including the competitive form of enzyme inhibitor, enzyme inhibition, the competitive form of receptor antagonist, receptor antagonism, the competitive form of antimetabolite activity, and the competitive form of poisoning (which can include any of the aforementioned types). Enzyme inhibition type In competitive inhibition of enzyme catalysis, binding of an inhibitor prevents binding of the target molecule of the enzyme, also known as the substrate. This is accomplished by blocking the binding site of the substrate – the active si ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Motion Sickness
Motion sickness occurs due to a difference between actual and expected motion. Symptoms commonly include nausea, vomiting, cold sweat, headache, dizziness, tiredness, loss of appetite, and increased salivation. Complications may rarely include dehydration, electrolyte problems, or a lower esophageal tear. The cause of motion sickness is either real or perceived motion. This may include car travel, air travel, sea travel, space travel, or reality simulation. Risk factors include pregnancy, migraines, and Ménière's disease. The diagnosis is based on symptoms. Treatment may include behavioral measures or medications. Behavioral measures include keeping the head still and focusing on the horizon. Three types of medications are useful: antimuscarinics such as scopolamine, H1 antihistamines such as dimenhydrinate, and amphetamines such as dexamphetamine. Side effects, however, may limit the use of medications. A number of medications used for nausea such as ondansetro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Journal Of Psychopharmacology
The ''Journal of Psychopharmacology'' is a monthly peer-reviewed scientific journal published by SAGE Publications on behalf of the British Association for Psychopharmacology. It was established in 1987 and is a member of the Committee on Publication Ethics. The editors-in-chief are David Nutt (Imperial College London) and Pierre Blier (University of Ottawa). The journal covers all aspects of psychopharmacology. Abstracting and indexing ''Journal of Psychopharmacology'' is abstracted and indexed in, among other databases: EMBASE/Excerpta Medica, MEDLINE, SCOPUS, and the Social Sciences Citation Index. According to the ''Journal Citation Reports'', the journal had a 2018 impact factor The impact factor (IF) or journal impact factor (JIF) of an academic journal is a type of journal ranking. Journals with higher impact factor values are considered more prestigious or important within their field. The Impact Factor of a journa ... of 4.738, ranking it 30 out of 197 journals ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyoscine Hydrobromide
Scopolamine, also known as hyoscine, or Devil's Breath, is a medication used to treat motion sickness and postoperative nausea and vomiting. It is also sometimes used before surgery to decrease saliva. When used by injection, effects begin after about 20 minutes and last for up to 8 hours. It may also be used orally and as a transdermal patch since it has been long known to have transdermal bioavailability. Scopolamine is in the antimuscarinic family of drugs and works by blocking some of the effects of acetylcholine within the nervous system. Scopolamine was first written about in 1881 and started to be used for anesthesia around 1900. Scopolamine is also the main active component produced by certain plants of the nightshade family, which historically have been used as psychoactive drugs, known as '' deliriants'', due to their antimuscarinic-induced hallucinogenic effects in higher doses. In these contexts, its mind-altering effects have been utilized for re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stroke
Stroke is a medical condition in which poor cerebral circulation, blood flow to a part of the brain causes cell death. There are two main types of stroke: brain ischemia, ischemic, due to lack of blood flow, and intracranial hemorrhage, hemorrhagic, due to bleeding. Both cause parts of the brain to stop functioning properly. Signs and symptoms of stroke may include an hemiplegia, inability to move or feel on one side of the body, receptive aphasia, problems understanding or expressive aphasia, speaking, dizziness, or homonymous hemianopsia, loss of vision to one side. Signs and symptoms often appear soon after the stroke has occurred. If symptoms last less than 24 hours, the stroke is a transient ischemic attack (TIA), also called a mini-stroke. subarachnoid hemorrhage, Hemorrhagic stroke may also be associated with a thunderclap headache, severe headache. The symptoms of stroke can be permanent. Long-term complications may include pneumonia and Urinary incontinence, loss of b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
