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PD-217,014
PD-217,014 is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α2δ calcium channels ( 1 and 2). It was developed as a potentially more potent successor to gabapentin and pregabalin Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anx ..., along with several other analogues such as atagabalin and 4-methylpregabalin, but while PD-217,014 produces visceral analgesic effects in animal studies with higher potency and efficacy than gabapentin, it was not developed further for clinical use because of its comparatively more complex synthesis, compared to other related analogues. References Abandoned drugs Analgesics Calcium channel blockers GABA analogues Gamma-Amino acids Drugs developed by Pfizer {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atagabalin
Atagabalin (PD-0200,390) is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α2δ calcium channels ( 1 and 2). It was under development as a treatment for insomnia, but was discontinued following unsatisfactory trial results. See also * 4-Methylpregabalin * Gabapentin enacarbil * PD-217,014 PD-217,014 is a drug developed by Pfizer and related to gabapentin, which similarly binds to the α2δ calcium channels ( 1 and 2). It was developed as a potentially more potent successor to gabapentin and pregabalin Pregabalin, sold under ... References Abandoned drugs Calcium channel blockers GABA analogues Gamma-Amino acids Hypnotics Drugs developed by Pfizer Cyclopentanes {{sedative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-methylpregabalin
4-Methylpregabalin is a drug developed by Pfizer and related to pregabalin, which similarly acts as an analgesic with effectiveness against difficult to treat "atypical" pain syndromes such as neuropathic pain. The effectiveness of pregabalin and its older relative gabapentin against pain syndromes of this kind (which tend to respond poorly to other analgesic drugs) has led to their widespread use, and these drugs have subsequently been found to be useful for many other medical applications, including as anticonvulsants, muscle relaxants, anxiolytics and mood stabilisers. However these drugs are still of relatively low potency, and scientists have struggled for years to come up with an improvement on pregabalin, with increasing pressure to find a suitably improved replacement before the patent on pregabalin expired in 2018. While it was determined that the mechanism of action involves modulation of the α2δ calcium channel subunits ( 1 and 2), derivatives that appeared to be m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pfizer
Pfizer Inc. ( ) is an American Multinational corporation, multinational Pharmaceutical industry, pharmaceutical and biotechnology corporation headquartered at The Spiral (New York City), The Spiral in Manhattan, New York City. Founded in 1849 in New York by German entrepreneurs Charles Pfizer (1824–1906) and Charles F. Erhart (1821–1891), Pfizer is one of the oldest pharmaceutical companies in North America. Pfizer develops and produces medicines and vaccines for immunology, oncology, cardiology, endocrinology, and neurology. The company's largest products by sales are the Pfizer–BioNTech COVID-19 vaccine ($11 billion in 2023 revenues), apixaban ($6 billion in 2023 revenues), a pneumococcal conjugate vaccine ($6 billion in 2023 revenues), palbociclib ($4 billion in 2023 revenues), and tafamidis ($3 billion in 2023 revenues). In 2023, 46% of the company's revenues came from the United States, 6% came from Japan, and 48% came from other countries. Pfizer has been a publi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gabapentin
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central pain. It is moderately effective: about 30–40% of those given gabapentin for diabetic neuropathy or postherpetic neuralgia have a meaningful benefit. Gabapentin, like other gabapentinoid drugs, acts by decreasing activity of the α2δ-1 protein, coded by the CACNA2D1 gene, first known as an auxiliary subunit of voltage gated calcium channels. However, see Pharmacodynamics, below. By binding to α2δ-1, gabapentin reduces the release of excitatory neurotransmitters (primarily glutamate) and as a result, reduces excess excitation of neuronal networks in the spinal cord and brain. Sleepiness and dizziness are the most common side effects. Serious side effects in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Calcium Channel
A calcium channel is an ion channel which shows selective permeability to calcium ions. It is sometimes synonymous with voltage-gated calcium channel, which are a type of calcium channel regulated by changes in membrane potential. Some calcium channels are regulated by the binding of a ligand.Striggow F, Ehrlich BE (August 1996). "Ligand-gated calcium channels inside and out". ''Current Opinion in Cell Biology''. 8 (4): 490–495. Doi (identifier), doi:doi:10.1016/S0955-0674(96)80025-1, 10.1016/S0955-0674(96)80025-1. PMID (identifier), PMID]8791458 Other calcium channels can also be regulated by both voltage and ligands to provide precise control over ion flow. Some cation channels allow calcium as well as other cations to pass through the membrane. Calcium channels can participate in the creation of Action potential, action potentials across cell membranes. Calcium channels can also be used to release calcium ions as Second messenger system, second messengers within the cell, affec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CACNA2D1
Voltage-dependent calcium channel subunit alpha-2/delta-1 is a protein that in humans is encoded by the ''CACNA2D1'' gene. This gene encodes a member of the alpha-2/delta subunit family, a protein in the voltage-dependent calcium channel complex. Calcium channels mediate the influx of calcium ions into the cell upon membrane depolarization and consist of a complex of alpha-1, alpha-2/delta, beta, and gamma subunits in a 1:1:1:1 ratio. Research on a highly similar protein in rabbit suggests the protein described in this record is cleaved into alpha-2 and delta subunits. Alternate transcriptional splice variants of this gene have been observed, but have not been thoroughly characterized. In mammals, alpha-2/delta proteins exist in four subtypes coded by four separate but closely related genes, CACNA2D1, CACNA2D2, CACNA2D3 and CACNA2D4. Recently, alpha-2/delta1 proteins, in addition to calcium channels, have been found to interact directly with N-methyl-D-aspartate type glutam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CACNA2D2
Voltage-dependent calcium channel subunit alpha2delta-2 is a protein that in humans is encoded by the ''CACNA2D2'' gene. This gene encodes a member of the alpha-2/delta subunit family, a protein in the voltage-dependent calcium channel complex. Calcium channels mediate the influx of calcium ions into the cell upon membrane polarization and consist of a complex of alpha-1, alpha-2/delta, beta, and gamma subunits in a 1:1:1:1 ratio. Various versions of each of these subunits exist, either expressed from similar genes or the result of alternative splicing. Research on a highly similar protein in rabbit suggests the protein described in this record is cleaved into alpha-2 and delta subunits. Alternate transcriptional splice variants of this gene, encoding different isoforms, have been characterized. CACNA2D2 containing channels are blocked by amiodarone. See also * Voltage-dependent calcium channel Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pregabalin
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anxiety disorder (GAD), and shingles. Pregabalin also has allodynia, antiallodynic properties. Its use in epilepsy is as an add-on therapy for partial seizures. When used before surgery, it reduces pain but results in greater sedation and visual disturbances. It is taken oral administration, by mouth. Common side effects can include headache, dizziness, somnolence, sleepiness, euphoria, confusion, trouble with memory, Ataxia, poor coordination, dry mouth, problems with vision, and weight gain. Serious side effects may include angioedema, kidney damage and drug misuse. As with all other drugs approved by the FDA for treating epilepsy, the pregabalin labeling warns of an increased suicide risk when combined with other drugs. When pregabalin i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aba ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, recent research has suggested that classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants may be considered as an alternative. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to the substantial risks and high chances of overdose, misuse, and addiction in the absence of medical supervision. Etymology The word ''analgesic'' derives ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Calcium Channel Blockers
Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium () through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients. Calcium channel blockers are also frequently used to alter heart rate (especially from atrial fibrillation), to prevent peripheral and cerebral vasospasm, and to reduce chest pain caused by angina pectoris. N-type, L-type, and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal gland, and CCBs can directly influence the biosynthesis of aldosterone in adrenocortical cells, with consequent impact on the clinical treatment of hypertension with these agents. CCBs have been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABA Analogues
GABA (gamma-aminobutyric acid, γ-aminobutyric acid) is the chief inhibitory neurotransmitter in the developmentally mature mammalian central nervous system. Its principal role is reducing neuronal excitability throughout the nervous system. GABA is sold as a dietary supplement in many countries. It has been traditionally thought that exogenous GABA (i.e., taken as a supplement) does not cross the blood–brain barrier, but data obtained from more recent research (2010s) in rats describes the notion as being unclear. The carboxylate form of GABA is γ-aminobutyrate. Function Neurotransmitter Two general classes of GABA receptor are known: * GABAA receptor, GABAA in which the receptor is part of a ligand-gated ion channel complex * GABAB receptor, GABAB metabotropic receptors, which are G protein-coupled receptors that open or close ion channels via intermediaries (G proteins) Neurons that produce GABA as their output are called GABAergic neurons, and have chiefly inhibito ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
