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Calcium channel blockers act on voltage-gated channels that let calcium ions enter excitable cells. Voltage-gated calcium (CaV) channels couple membrane depolarization to muscle contraction, neurotransmitter release and gene expression. Channel types are classed as L-, N-, P/Q-, R- and T-type according to their electrophysiological and pharmacological properties. The pore-forming α1 subunit of the L-type channel was first sequenced in 1987 as the skeletal muscle receptor for calcium channel blockers. Dihydropyridines in this category include isradipine, nimodipine and amlodipine besylate, which bind L-type channels. The benzothiazepine diltiazem HCl acts on the same channel type at a distinct binding site. BAPTA/AM, the cell-permeant ester of a calcium chelator, is listed for buffering intracellular calcium rather than for blocking channels.
Synonyms: DS 5565 besylate; DS5565
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
Synonyms: DS5565
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
Synonyms: 2-Hydroxyethanesulfonic acid
Isethionic acid is a calcium binder that functions by competitively occupying calcium binding sites on the outer mitochondrial membrane, thereby enhancing mitochondrial calcium binding capacity. This compound inhibits calcium-activated mitochondrial respiration and demonstrates significant biological activity by affecting barnacle (Balanus amphitrite) larvae with LC50 values of 23 µg/mL at 24 hours and 17 µg/mL at 48 hours. Isethionic acid effectively prevents the attachment of barnacle larvae at concentrations as low as 10 µg/mL and regulates mitochondrial calcium transport, promoting ATP-dependent calcium uptake in high calcium environments. This reagent is valuable for investigations into mitochondrial calcium metabolism mechanisms.
Synonyms: HSK16149
Crisugabalin is a selective ligand targeting the α2δ subunit of voltage-gated calcium channels, exhibiting an IC50 of 3.96 nM in rat models. This compound effectively inhibits the binding of [3H]gabapentin to the α2δ subunit, leading to reduced calcium influx and decreased neuronal excitability, ultimately impairing nociceptive transmission. Crisugabalin has demonstrated efficacy in alleviating mechanical allodynia and various pain models, including neuropathic and inflammatory pain. Its applications are relevant in research contexts involving chronic pain syndromes such as diabetic neuropathy, fibromyalgia, and postherpetic neuralgia.
PD-217014 is an α2δ ligand targeting calcium channels, demonstrating significant visceral analgesic activity. This compound effectively inhibits visceral hypersensitivity reactions, exhibiting a dose-dependent anti-allodynic effect. It serves as a valuable tool in research related to pain management and the mechanisms underlying visceral pain.
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PD-0299685 is a potent ligand for the Ca2+ channel α2δ subunit. This compound exhibits significant potential in the study of refractory genito-urinary pain conditions, including interstitial cystitis and bladder pain syndrome. Its ability to modulate calcium channel activity makes it a valuable tool in pain research and related therapeutic investigations.
Synonyms: PD-0332334
β-Amino Acid Imagabalin Hydrochloride is a selective ligand for the α2δ subunit of voltage-dependent calcium channels. This compound modulates calcium influx, thereby regulating neurotransmitter release and exhibiting anticonvulsant properties. It is primarily utilized in research focused on pain management, anxiety disorders, and seizure activity.
α2δ ligand 1 selectively interacts with the α2δ-1 subunit of voltage-gated calcium channels. This compound is known to modulate calcium influx, which plays a crucial role in neuronal excitability and synaptic transmission. It is utilized in research applications focused on pain management, neurological disorders, and the exploration of synaptic plasticity.
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