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Biological Activity for ZD 7288
ZD 7288 is a sino-atrial node function modulator; blocks the hyperpolarization activated cation current If (HCN channel). Blocks Ih in central neurons. Increases NMDA-evoked noradrenaline release in rat brain in vitro.
Sold with the permission of AstraZeneca UK Ltd.
Compound Libraries for ZD 7288
Technical Data for ZD 7288
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ZD 7288
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for ZD 7288
The following data is based on the product molecular weight 292.81. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.42 mL||17.08 mL||34.15 mL|
|5 mM||0.68 mL||3.42 mL||6.83 mL|
|10 mM||0.34 mL||1.71 mL||3.42 mL|
|50 mM||0.07 mL||0.34 mL||0.68 mL|
References for ZD 7288
References are publications that support the biological activity of the product.
BoSmith et al (1993) Inhibitory actions of ZENECA ZD7288 on whole cell hyperpolarization activated inward current (If) in guinea-pig dissociated sinoatrial node cells. Br.J.Pharmacol. 110 343 PMID: 7693281
Green et al (1996) Pharmacological characterization of the inwardly rectifying current in the smooth muscle cells of the rat bladder. Br.J.Pharmacol. 119 1509 PMID: 8982495
Harris and Constanti (1995) Mechanism of block by ZD7288 of the hyperpolarization-activated inward rectifying current in guinea-pig substantia nigra neurons in vitro. J.Neurophysiol. 74 2366 PMID: 8747199
Klar et al (2003) Ih channels as modulators of presynaptic terminal function: ZD7288 increases NMDA-evoked [3H]-noradrenaline release in rat neocortex slices. Naunyn Schmiedebergs Arch.Pharmacol. 367 422 PMID: 12690435
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Keywords: ZD 7288, ZD 7288 supplier, Sino-atrial, node, function, modulators, If, inhibitors, inhibits, Channel, VDAC, ZD7288, ICID7288, AstraZeneca, HCN, ICI, D7288, Channels, 1000, Tocris Bioscience
54 Citations for ZD 7288
Citations are publications that use Tocris products. Selected citations for ZD 7288 include:
Lopez et al (2022) Ketamine exerts its sustained antidepressant effects via cell-type-specific regulation of Kcnq2. Neuron 110 2283 PMID: 35649415
Collins et al (2018) Reciprocal Circuits Linking the Prefrontal Cortex with Dorsal and Ventral Thalamic Nuclei. Neuron 98 366 PMID: 29628187
Harris et al (2018) Dorsal BNST α2A-Adrenergic Receptors Produce HCN-Dependent Excitatory Actions That Initiate Anxiogenic Behaviors. J Neurosci 38 8922 PMID: 30150361
Ghezzi et al (2016) Electrophysiological characterization of the M-current in rat hypoglossal motoneurons Neuroscience 340 62 PMID: 27984184
Fan et al (2016) Reduced Hyperpolarization-Activated Current Contributes to Enhanced Intrinsic Excitability in Cultured Hippocampal Neurons from PrP(-/-) Mice. Front Cell Neurosci 10 74 PMID: 27047338
Zhong and Zucker (2005) cAMP acts on exchange protein activated by cAMP/cAMP-regulated guanine nucleotide exchange protein to regulate transmitter release at the crayfish neuromuscular junction. J Neurosci 25 208 PMID: 15634783
Adachi et al (2005) Noradrenergic modulation of XII motoneuron inspiratory activity does not involve alpha2-receptor inhibition of the Ih current or presynaptic glutamate release. J Appl Physiol (1985) 98 1297 PMID: 15579572
Flynn and Zagotta (2018) Insights into the molecular mechanism for hyperpolarization-dependent activation of HCN channels. Proc Natl Acad Sci U S A 115 E8086 PMID: 30076228
Kashyap et al (2015) Characterization of the role of HCN channels in β3-adrenoceptor mediated rat bladder relaxation. Front Cell Neurosci 2 PMID: 26709376
Ferreira et al (2015) Highly differentiated cellular and circuit properties of infralimbic pyramidal neurons projecting to the periaqueductal gray and amygdala. PLoS One 9 161 PMID: 25972785
Ohno et al (2015) Hcn1 is a tremorgenic genetic component in a rat model of essential tremor. J Neurosci 10 e0123529 PMID: 25970616
Boehlen et al (2013) Contribution of near-threshold currents to intrinsic oscillatory activity in rat medial entorhinal cortex layer II stellate cells. J Neurophysiol 109 445 PMID: 23076110
Zhang et al (2013) NE drives persistent activity in prefrontal cortex via synergistic α1 and α2 adrenoceptors. PLoS One 8 e66122 PMID: 23785477
Yi et al (2013) Contribution of d1/5 receptor modulation of post-spike/burst afterhyperpolarization to enhance neuronal excitability of layer v pyramidal neurons in prepubertal rat prefrontal cortex. PLoS One 8 e71880 PMID: 23977170
Masi et al (2013) MPP(+) -dependent inhibition of Ih reduces spontaneous activity and enhances EPSP summation in nigral DA neurons. Br J Pharmacol 169 130 PMID: 23323755
Gullo et al (2010) Orchestration of "presto" and "largo" synchrony in up-down activity of cortical networks. Front Neural Circuits 4 11 PMID: 20461235
Chu et al (2010) Electrophysiological effects of SKF83959 on hippocampal CA1 pyramidal neurons: potential mechanisms for the drug's neuroprotective effects. PLoS One 5 PMID: 20957037
Doan et al (2004) Differential distribution and function of hyperpolarization-activated channels in sensory neurons and mechanosensitive fibers. Brain 24 3335 PMID: 15056713
Hegg and Lucero (2004) DA reduces odor- and elevated-K(+)-induced calcium responses in mouse olfactory receptor neurons in situ. J Neurophysiol 91 1492 PMID: 14657189
Seeburg et al (2004) Frequency-dependent modulation of retinogeniculate transmission by serotonin. J Neurosci 24 10950 PMID: 15574745
Brummett et al (2011) Perineural dexmed. added to ropiva. for sciatic nerve block in rats prolongs the duration of analgesia by blocking the hyperpolarization-activated cation current. Anesthesiology 115 836 PMID: 21666435
Gill et al (2004) Characterization of the human HCN1 channel and its inhibition by capsazepine. Br J Pharmacol 143 411 PMID: 15351778
Chan et al (2004) HCN2 and HCN1 channels govern the regularity of autonomous pacemaking and synaptic resetting in globus pallidus neurons. J Neurosci 24 9921 PMID: 15525777
Lezmy (2017) M-current inhibition rapidly induces a unique CK2-dependent plasticity of the axon initial segment. Proc Natl Acad Sci U S A 114 E10234 PMID: 29109270
Williams and Hablitz (2015) Differential modulation of repetitive firing and synchronous network activity in neocortical interneurons by inhibition of A-type K(+) channels and Ih. Front Cell Neurosci 9 89 PMID: 25852481
Dragicevic et al (2014) Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra DA neurons. Bladder (San Franc) 137 2287 PMID: 24934288
Abbas et al (2013) Directional summation in non-direction selective retinal ganglion cells. PLoS Comput Biol 9 e1002969 PMID: 23516351
Stark et al (2013) Inhibition-induced theta resonance in cortical circuits. Neuron 80 1263 PMID: 24314731
Zhang et al (2013) Molecular mechanisms that drive E2-dependent burst firing of Kiss1 neurons in the rostral periventricular preoptic area. Am J Physiol Endocrinol Metab 305 E1384 PMID: 24105416
Atkinson et al (2011) Cyclic AMP signaling control of action potential firing rate and molecular circadian pacemaking in the suprachiasmatic nucleus. J Biol Rhythms 26 210 PMID: 21628548
Ballo and Bucher (2009) Complex intrinsic membrane properties and DA shape spiking activity in a motor axon. J Neurosci 29 5062 PMID: 19386902
Bal and Baydas (2009) Electrophysiological properties of octopus neurons of the cat cochlear nucleus: an in vitro study. J Assoc Res Otolaryngol 10 281 PMID: 19277784
Zhang et al (2009) Developmental expression of a functional TASK-1 2P domain K+ channel in embryonic chick heart. J Neurosci 16 104 PMID: 19930646
Molineux et al (2008) Ionic factors governing rebound burst phenotype in rat deep cerebellar neurons. Cereb Cortex 100 2684 PMID: 18768644
Zhao et al (2018) Soluble Aβ Oligomers Impair Dipolar Heterodendritic Plasticity by Activation of mGluR in the Hippocampal CA1 Region. iScience 6 138 PMID: 30240608
Asteriti et al (2015) A Cambrian origin for vertebrate rods. Elife 4 PMID: 26095697
Calejo et al (2014) Hyperpolarization-activated cyclic nucleotide-gated channels and cAMP-dependent modulation of exocytosis in cultured rat lactotrophs. J Neurosci 34 15638 PMID: 25411492
Safiulina et al (2008) Low expression of Kv7/M channels facilitates intrinsic and network bursting in the developing rat hippocampus. J Physiol 586 5437 PMID: 18801845
Russo et al (2008) Dynamic metabotropic control of intrinsic firing in cerebellar unipolar brush cells. J Neurophysiol 100 3351 PMID: 18945818
Patel et al (2012) Frequency-selective exocytosis by ribbon synapses of hair cells in the bullfrog's amphibian papilla. Exp Physiol 32 13433 PMID: 23015434
Ma et al (2011) High purity human-induced pluripotent stem cell-derived cardiomyocytes: electrophysiological properties of action potentials and ionic currents. J Biomed Sci 301 H2006 PMID: 21890694
Goldberg et al (2011) Rapid developmental maturation of neocortical FS cell intrinsic excitability. J Neurosci 21 666 PMID: 20705896
Brager and Johnston (2007) Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons. J Neurosci 27 13926 PMID: 18094230
Lee and Ishida (2007) Ih without Kir in adult rat retinal ganglion cells. J Neurophysiol 97 3790 PMID: 17488978
Lee and Tepper (2007) A calcium-activated nonselective cation conductance underlies the plateau potential in rat substantia nigra GABAergic neurons. J Neurosci 27 6531 PMID: 17567814
Bender et al (2007) Localization of HCN1 channels to presynaptic compartments: novel plasticity that may contribute to hippocampal maturation. J Neurosci 27 4697 PMID: 17460082
Zhang et al (2018) Pauses in Cholinergic Interneuron Activity Are Driven by Excitatory Input and Delayed Rectification, with DA Modulation. Neuron 98 918 PMID: 29754751
Cilz et al (2014) DA modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels. Cereb Cortex 24 3195 PMID: 23843440
Angelo and Margrie (2012) Population diversity and function of hyperpolarization-activated current in olfactory bulb mitral cells. Sci Rep 1 50 PMID: 22355569
Few et al (2012) Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release. Proc Natl Acad Sci U S A 109 E452 PMID: 22308469
Jung et al (2010) Downregulation of dendritic HCN channel gating in epilepsy is mediated by altered phosphorylation signaling. J Neurosci 30 6678 PMID: 20463230
Chen et al (2010) Homeostatic regulation of synaptic excitability: tonic GABA(A) receptor currents replace I(h) in cortical pyramidal neurons of HCN1 knock-out mice. J Neurosci 30 2611 PMID: 20164346
Narushima et al (2007) Tonic enhancement of endocannabinoid-mediated retrograde suppression of inhibition by cholinergic interneuron activity in the striatum. PLoS One 27 496 PMID: 17234582
Angelo et al (2007) Local and global effects of I(h) distribution in dendrites of mammalian neurons. Am J Physiol Heart Circ Physiol 27 8643 PMID: 17687042
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We used ZD-7288 to block Ih current in hippocampal pyramidal cells. 10 µM concentration of the compound developed its effect within a characteristic time interval of tens of seconds, making slower decay kinetics of evoked post-synaptic potentials (see illustration). Washout for 15-20 minutes could not restore the control response characteristics, thus suggesting high affinity of the compound.
No problem with dissolution in water and preparation of 10 mM stock.
Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.