Calcium channel opener
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
- Calcium channel blocker
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.
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Pharmacomodulation
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Partial agonist
- Antagonist
- Inverse agonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- ♦ Miscellaneous: Precursor
- Cofactor
| Enzyme | see Enzyme inhibition |
|---|---|
| Ion channel | See Ion channel modulators |
| Receptor & transporter | |
| Miscellaneous |
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