A calcium channel opener is a type of drug which facilitates ion transmission through calcium channels.
An example is Bay K8644, which is an analogue of nifedipine that specifically and directly activates L-type voltage-dependent calcium channels.[1]
In contrast to Bay K8644, which is not for clinical use, ambroxol is a frequently used mucolytic drug that triggers lysosomal secretion by mobilizing calcium from acidic calcium stores.[2] This effect does most likely not occur by a direct interaction between the drug and a lysosomal calcium channel, but indirectly by neutralizing the acidic pH within lysosomes. Calcium permeable ion channels in lysosomal membranes that may be activated by a luminal pH increase include two pore channels (TPCs), mucolipin TRP channels (TRPMLs) and purinergic receptors of the P2X channel type.[3][4]
See also
References
- ^ Schramm M, Thomas G, Towart R, Franckowiak G (1983). "Activation of calcium channels by novel 1,4-dihydropyridines. A new mechanism for positive inotropics or smooth muscle stimulants". Arzneimittelforschung. 33 (9): 1268–72. PMID 6196037.
- ^ Fois, Giorgio; Hobi, Nina; Felder, Edward; Ziegler, Andreas; Miklavc, Pika; Walther, Paul; Radermacher, Peter; Haller, Thomas; Dietl, Paul (2015). "A new role for an old drug: Ambroxol triggers lysosomal exocytosis via pH-dependent Ca2+ release from acidic Ca2+ stores". Cell Calcium. 58 (6): 628–637. doi:10.1016/j.ceca.2015.10.002. PMID 26560688.
- ^ Patel, Sandip; Cai, Xinjiang (2015). "Evolution of acidic Ca2+ stores and their resident Ca2+-permeable channels". Cell Calcium. 57 (3): 222–230. doi:10.1016/j.ceca.2014.12.005. PMID 25591931.
- ^ Xu, Haoxing; Ren, Dejian (2015-01-01). "Lysosomal Physiology". Annual Review of Physiology. 77 (1): 57–80. doi:10.1146/annurev-physiol-021014-071649. PMC 4524569. PMID 25668017.
Pharmacomodulation |
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| Types |
- ♦ Receptor: Agonist
- Partial agonist
- Antagonist
- Inverse agonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
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| Classes | | Enzyme | see Enzyme inhibition |
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| Ion channel | See Ion channel modulators |
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Receptor & transporter | | BA/M | | Adrenergic | |
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| Dopaminergic | |
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| Histaminergic | |
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| Serotonergic |
- Serotonin receptor agonist
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- Serotonin reuptake inhibitor (SRI)
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| AA | | GABAergic | |
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| Glutamatergic |
- Glutamate receptor agonist (AMPA)
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- Glutamate reuptake inhibitor
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| Cholinergic |
- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
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- Nicotinic (Ganglionic
- Muscular))
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| Cannabinoidergic |
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- Endocannabinoid reuptake inhibitor (eCBRI)
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| Opioidergic |
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- Enkephalinase inhibitor
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| Other |
- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
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| Miscellaneous | |
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Ion channel modulators |
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| Calcium | | VDCCsTooltip Voltage-dependent calcium channels | |
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| Potassium | |
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| Sodium | | VGSCsTooltip Voltage-gated sodium channels | | Blockers |
- Antiarrhythmics (class I): Ajmaline
- Aprindine
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- Local anesthetics: pFBT
- Amylocaine
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- Analgesics: AZD-3161
- DSP-2230
- Funapide
- GDC-0276
- NKTR-171
- PF-04531083
- PF-05089771
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- RG7893 (GDC-0287)
- Suzetrigine
- Others: Buprenorphine
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- Safinamide
- Tricyclic antidepressants
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| ENaCTooltip Epithelial sodium channel | | Blockers |
- Amiloride
- Benzamil
- Triamterene
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| Activators | |
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| ASICsTooltip Acid-sensing ion channel | | Blockers |
- A-317567
- Amiloride
- Aspirin
- Ibuprofen
- PcTX1
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| Chloride | | CaCCsTooltip Calcium-activated chloride channel | | Blockers |
- Crofelemer
- DIDS
- Ethacrynic acid
- Flufenamic acid
- Fluoxetine
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- Glibenclamide
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| Activators | |
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| CFTRTooltip Cystic fibrosis transmembrane conductance regulator | | Blockers |
- Glibenclamide
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| Activators |
- 1,7-Phenanthroline
- 1,10-Phenanthroline
- 4,7-Phenanthroline
- 7,8-Benzoquinoline
- Ivacaftor
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| Unsorted | | Blockers |
- Bumetanide
- Flufenamic acid
- Meclofenamic acid
- Mefenamic acid
- Mepacrine
- Niflumic acid
- Talniflumate
- Tolfenamic acid
- Trifluoperazine
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| Others | | TRPsTooltip Transient receptor potential channels | |
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| LGICsTooltip Ligand gated ion channels | |
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See also: Receptor/signaling modulators • Transient receptor potential channel modulators |