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Submit Review8-Hydroxy-DPAT hydrobromide
Description: Selective 5-HT1A agonist; also has moderate affinity for 5-HT7
Alternative Names: 8-OH-DPAT hydrobromide
Chemical Name: (±)-8-Hydroxy-2-dipropylaminotetralin hydrobromide
Purity: ≥98% (HPLC)
Biological Activity for 8-Hydroxy-DPAT hydrobromide
The standard selective 5-HT1A agonist. Also has moderate affinity for 5-HT7 receptors (pKi is 6.6 at the human 5-HT7 receptor expressed in HEK 293 cells). Reduces hippocampal 5-HT levels following systemic administration in rats in vivo.
R-enantiomer and 7-Hydroxy Isomer also available..
Technical Data for 8-Hydroxy-DPAT hydrobromide
| M. Wt | 328.29 |
| Formula | C16H25NO.HBr |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 76135-31-4 |
| PubChem ID | 6917794 |
| InChI Key | BATPBOZTBNNDLN-UHFFFAOYSA-N |
| Smiles | Br.CCCN(CCC)C1CCC2=CC=CC(O)=C2C1 |
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.
Product Datasheets for 8-Hydroxy-DPAT hydrobromide
References for 8-Hydroxy-DPAT hydrobromide
References are publications that support the biological activity of the product.
Helton and Colbert (1994) Alteration of in-vitro 5-HT receptor pharmacology as a function of multiple treatment with 5-hydroxytryptamine of 8-hydroxy-2-(di-N-propylamino)tetralin in rat isolated aorta, uterus and fundus, and guinea pig isolated trachea. J.Pharm.Pharmacol. 46 902 PMID: 7897596
Middlemiss et al (1983) 8-OH-DPAT discriminates between subtypes of the 5HT1 recognition site. Eur.J.Pharmacol. 90 151 PMID: 6223827
Wood et al (2000) Antagonist activity of meta-chlorophenylpiperazine and partial agonist activity of 8-OH-DPAT at the 5-HT7 receptor. Eur.J.Pharmacol. 396 1 PMID: 10822046
Yoshitake and Kehr (2004) Differential effects of (R)-, (R, S)- and (S)-8-hydroxy-2-(di-n-propylamino)tetralin on hippocampal serotonin release and induction of hypothermia in awake rats. Life Sci. 74 2865 PMID: 15050424
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Keywords: 8-Hydroxy-DPAT hydrobromide, 8-Hydroxy-DPAT hydrobromide supplier, moderate, affinity, 5-HT7, 5-HT1A, agonists, Selective, Serotonin, Receptors, 5-Hydroxytryptamine, 5-HT1, 8-OH-DPAT, hydrobromide, 0529, Tocris Bioscience
28 Citations for 8-Hydroxy-DPAT hydrobromide
Citations are publications that use Tocris products. Selected citations for 8-Hydroxy-DPAT hydrobromide include:
Majeed et al (2016) Modulatory Action by the Serotonergic System: Behavior and Neurophysiology in Drosophila melanogaster. Neural Plast 2016 7291438 PMID: 26989517
Rock et al (2012) Cannabidiol, a non-psychotropic component of cannabis, attenuates vomiting and nausea-like behaviour via indirect agonism of 5-HT(1A) somatodendritic autoreceptors in the dorsal raphe nucleus. Br J Pharmacol 165 2620 PMID: 21827451
Borroto-Escuela et al (2012) The existence of FGFR1-5-HT1A receptor heterocomplexes in midbrain 5-HT neurons of the rat: relevance for neuroplasticity. J Neurosci 32 6295 PMID: 22553035
Ishima et al (2012) Neurite outgrowth mediated by the heat shock protein Hsp90α: a novel target for the antipsychotic drug aripipr. Transl Psychiatry 2 e170 PMID: 23047241
Manzke et al (2010) Serotonin receptor 1A-modulated phosphorylation of glycine receptor α3 controls breathing in mice. J Clin Invest 120 4118 PMID: 20978350
Hensler et al (2010) Regulation of cortical and hippocampal 5-HT(1A) receptor function by corticosterone in GR+/- mice. Psychoneuroendocrinology 35 469 PMID: 19766402
Rawls et al (2010) 5-HT(1A)-like receptor activation inhibits abstinence-induced metha. withdrawal in planarians. Neurosci Lett 484 113 PMID: 20709144
Maciag et al (2006) Evidence that the deficit in sexual behavior in adult rats neonatally exposed to cital. is a consequence of 5-HT1 receptor stimulation during development. Brain Res 1125 171 PMID: 17101120
McAllister et al (2014) GPER1 stimulation alters posttranslational modification of RGSz1 and induces desensitization of 5-HT1A receptor signaling in the rat hypothalamus. Neuroendocrinology 100 228 PMID: 25402859
Bonchak et al (2014) Targeting melanocyte and melanoma stem cells by 8-hydroxy-2-dipropylaminotetralin. Arch Biochem Biophys 563 71 PMID: 25132642
Duncan et al (2010) The effects of aging and chronic fluox. treatment on circadian rhythms and suprachiasmatic nucleus expression of neuropeptide genes and 5-HT1B receptors. J Pharmacol Exp Ther 31 1646 PMID: 20525077
Shelton et al (2015) Selective pharmacological blockade of the 5-HT7 receptor attenuates light and 8-OH-DPAT induced phase shifts of mouse circadian wheel running activity. Front Behav Neurosci 8 453 PMID: 25642174
Khatri et al (2014) Lasting neurobehavioral abnormalities in rats after neonatal activation of serotonin 1A and 1B receptors: possible mechanisms for serotonin dysfunction in autistic spectrum disorders. Psychopharmacology (Berl) 231 1191 PMID: 23975037
Walory et al (2018) Oncotoxic Properties of Serotonin Transporter Inhibitors and 5-HT1A Receptor Ligands. Int J Mol Sci 19 PMID: 30347827
Fuss et al (2013) Hippocampal serotonin-1A receptor function in a mouse model of anxiety induced by long-term voluntary wheel running. Synapse 67 648 PMID: 23505009
Araragi et al (2013) Conservation of 5-HT1A receptor-mediated autoinhibition of serotonin (5-HT) neurons in mice with altered 5-HT homeostasis. Front Pharmacol 4 97 PMID: 23935583
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
Manzke et al (2009) Serotonin targets inhibitory synapses to induce modulation of network functions. Philos Trans R Soc Lond B Biol Sci 364 2589 PMID: 19651659
Müller et al (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One 4 e6453 PMID: 19649285
Pagano et al (2008) Gαo/i-stimulated proteosomal degradation of RGS20: a mechanism for temporal integration of Gs and Gi pathways. J Neurosci 20 1190 PMID: 18407463
Gadgaard & Jensen (2020) Functional characterization of 5-HT1A and 5-HT1B serotonin receptor signaling through G-protein-activated inwardly rectifying K+ channels in a fluorescence-based membrane potential assay. Biochem Pharmacol 175 PMID: 32088264
Richardson and Shelton (2015) N-MthD.-aspartate receptor channel blocker-like discriminative stimulus effects of nitrous oxide gas. Cell Signal 352 156 PMID: 25368340
Watts et al (2015) 5-HT is a potent relaxant in rat superior mesenteric veins. Invest Ophthalmol Vis Sci 3 e00103 PMID: 25692021
Tullis et al (2015) Sarpogrelate, a 5-HT2A Receptor Antagonist, Protects the Retina From Light-Induced Retinopathy. Eur J Neurosci 56 4560 PMID: 26200496
Rossi et al (2010) OE-induced desensitization of 5-HT1A receptor signaling in the paraventricular nucleus of the hypothalamus is independent of estrogen receptor-beta. Psychoneuroendocrinology 35 1023 PMID: 20138435
Nguyen et al (2019) Potentiation of the glycine response by serotonin on the substantia gelatinosa neurons of the trigeminal subnucleus caudalis in mice. Korean J Physiol Pharmacol 23 271 PMID: 31297011
Carvalho-Dias (2017) Serotonin regulates prostate growth through androgen receptor modulation. Sci Rep 7 15428 PMID: 29133842
Yin et al (2017) Selective Modulation of Axonal Sodium Channel Subtypes by 5-HT1A Receptor in Cortical Pyramidal Neuron. Cereb Cortex 27 509 PMID: 26494800
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5-HT has a potential for relaxant.
By
Anonymous on 02/18/2020
Assay Type: In Vivo
Species: Rat
5-HT1A/7 receptor (8-OHDPAT)(0.1 lmol/L)
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