ArticleBritish journal of pharmacology2004
Characterization of the human HCN1 channel and its inhibition by capsazepine.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers, 1 of them a synthesis that pooled it.
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Who cites it
21 citing papers in PubMed, 1 synthesis or guideline pooled it, 53 citations in OpenAlex.
- The Contribution of HCN Channelopathies in Different Epileptic Syndromes, Mechanisms, Modulators, and Potential Treatment Targets: A Systematic Review.Frontiers in molecular neuroscience · 2022Pooled it
- A Comparative Study of the Antiemetic Effects of αInternational journal of molecular sciences · 2024Article
- Transient Receptor Potential (TRP) Ion Channels in Orofacial Pain.Molecular neurobiology · 2021Review
- Central Amygdala Projections to Lateral Hypothalamus Mediate Avoidance Behavior in Rats.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2021Article
- Physiology and Therapeutic Potential of SK, H, and M Medium AfterHyperPolarization Ion Channels.Frontiers in molecular neuroscience · 2021Review
- The HCN Channel Blocker ZD7288 Induces Emesis in the Least Shrew (Frontiers in pharmacology · 2021Article
- Identification and characterization of a series of novel HCN channel inhibitors.Acta pharmacologica Sinica · 2019Article
- TRPV1 channels contribute to spontaneous glutamate release in nucleus tractus solitarii following chronic intermittent hypoxia.Journal of neurophysiology · 2019Article
- Possible involvement of peripheral TRP channels in the hydrogen sulfide-induced hyperalgesia in diabetic rats.BMC neuroscience · 2019Article
- Article
- Identification of capsazepine as a novel inhibitor of system xJournal of pain research · 2017Article
- Essential roles of AMPA receptor GluA1 phosphorylation and presynaptic HCN channels in fast-acting antidepressant responses of ketamine.Science signaling · 2016Article
- HCN Channels Modulators: The Need for Selectivity.Current topics in medicinal chemistry · 2016Review
- Acid-sensing hypothalamic neurons controlling arousal.Cellular and molecular neurobiology · 2014Review
- Presynaptic HCN1 channels regulate Cav3.2 activity and neurotransmission at select cortical synapses.Nature neuroscience · 2011Article
- The transient receptor potential vanilloid-1 channel in thermoregulation: a thermosensor it is not.Pharmacological reviews · 2009Review
- The role of transient receptor potential vanilloid 1 in mechanical and chemical visceral hyperalgesia following experimental colitis.Neuroscience · 2007Article
- Analgesic actions of N-arachidonoyl-serotonin, a fatty acid amide hydrolase inhibitor with antagonistic activity at vanilloid TRPV1 receptors.British journal of pharmacology · 2007Article
- Dual stretch responses of mHCN2 pacemaker channels: accelerated activation, accelerated deactivation.Biophysical journal · 2007Article
- Regulation of recombinant and native hyperpolarization-activated cation channels.Molecular neurobiology · 2004Review
Corrections and comments
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Authors and funding
13 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The human hyperpolarization-activated cyclic nucleotide-gated 1 (hHCN1) subunit was heterologously expressed in mammalian cell lines (CV-1 and CHO) and its properties investigated using whole-cell patch-clamp recordings. Activation of this recombinant channel, by membrane hyperpolarization, generated a slowly activating, noninactivating inward current. The pharmacological properties of hHCN1-mediated currents resembled those of native hyperpolarization-activated currents (I(h)), that is, blockade by Cs(+) (99% at 5 mm), ZD 7288 (98% at 100 microm) and zatebradine (92% at 10 microm). Inhibition of the hHCN1-mediated current by ZD 7288 was apparently independent of prior channel activation (i.e. non-use-dependent), whereas that induced by zatebradine was use-dependent. The VR1 receptor antagonist capsazepine inhibited hHCN1-mediated currents in a concentration-dependent (IC(50)=8 microm), reversible and apparently non-use-dependent manner. This inhibitory effect of capsazepine was voltage-independent and associated with a leftward shift in the hHCN1 activation curve as well as a dramatic slowing of the kinetics of current activation. Elevation of intracellular cAMP or extracellular K(+) significantly enhanced aspects of hHCN1 currents. However, these manipulations did not significantly affect the capsazepine-induced inhibition of hHCN1. The development of structural analogues of capsazepine may yield compounds that could selectively inhibit HCN channels and prove useful for the treatment of neurological disorders where a role for HCN channels has been described.
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