8-Hydroxy-DPAT hydrobromide

Name: 8-Hydroxy-DPAT hydrobromide
Brand: Tocris Bioscience
SKU: 0529
Rating: 5 (1 reviews)

Catalog # 0529

Citations (28)

(1)

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Key Product Details

Description:	Selective 5-HT_1A agonist; also has moderate affinity for 5-HT₇
Alternative Names:	8-OH-DPAT hydrobromide
Chemical Name:	(±)-8-Hydroxy-2-dipropylaminotetralin hydrobromide
Purity:	≥98% (HPLC)
Molecular Weight:	328.29

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Biological Activity

The standard selective 5-HT_1A agonist. Also has moderate affinity for 5-HT₇ receptors (pK_i 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

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	3.28	10 with gentle warming
	DMSO	16.41	50

Preparing Stock Solutions

The following data is based on the product molecular weight 328.29.

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.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	6.09 mL	30.46 mL	60.92 mL
2.5 mM	1.22 mL	6.09 mL	12.18 mL
5 mM	0.61 mL	3.05 mL	6.09 mL
25 mM	0.12 mL	0.61 mL	1.22 mL

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References

References are publications that support the biological activity of the product.

Yoshitake and Kehr 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. 2004 PMID: 15050424
Wood Antagonist activity of meta-chlorophenylpiperazine and partial agonist activity of 8-OH-DPAT at the 5-HT₇ receptor. Eur.J.Pharmacol. 2000 PMID: 10822046
Helton and Colbert 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. 1994 PMID: 7897596
Middlemiss 8-OH-DPAT discriminates between subtypes of the 5HT₁ recognition site. Eur.J.Pharmacol. 1983 PMID: 6223827

Citations for 8-Hydroxy-DPAT hydrobromide (28)

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Citations are publications that use Bio-Techne products. Selected citations for 8-Hydroxy-DPAT hydrobromide include:

Gadgaard & Jensen (2020) Functional characterization of 5-HT_1A and 5-HT_1B serotonin receptor signaling through G-protein-activated inwardly rectifying K⁺ channels in a fluorescence-based membrane potential assay. Biochem Pharmacol. 175
PMID: 32088264
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
Walory et al. (2018) Oncotoxic Properties of Serotonin Transporter Inhibitors and 5-HT1A Receptor Ligands. Int J Mol Sci. 19
PMID: 30347827
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
Carvalho-Dias (2017) Serotonin regulates prostate growth through androgen receptor modulation. Sci Rep. 7(1):15428
PMID: 29133842
Majeed et al. (2016) Modulatory Action by the Serotonergic System: Behavior and Neurophysiology in Drosophila melanogaster. Neural Plast. 2016:7291438
PMID: 26989517
Watts et al. (2015) 5-HT is a potent relaxant in rat superior mesenteric veins. Invest Ophthalmol Vis Sci. 3:e00103
PMID: 25692021
Richardson and Shelton (2015) N-MthD.-aspartate receptor channel blocker-like discriminative stimulus effects of nitrous oxide gas. Cell Signal. 352:156
PMID: 25368340
Tullis et al. (2015) Sarpogrelate, a 5-HT2A Receptor Antagonist, Protects the Retina From Light-Induced Retinopathy. Eur J Neurosci. 56:4560
PMID: 26200496
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
Bonchak et al. (2014) Targeting melanocyte and melanoma stem cells by 8-hydroxy-2-dipropylaminotetralin. Arch Biochem Biophys. 563:71
PMID: 25132642
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
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
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
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
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
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
Manzke et al. (2010) Serotonin receptor 1A-modulated phosphorylation of glycine receptor α3 controls breathing in mice. J Clin Invest. 120:4118
PMID: 20978350
Rawls et al. (2010) 5-HT(1A)-like receptor activation inhibits abstinence-induced metha. withdrawal in planarians. Neurosci Lett. 484:113
PMID: 20709144
Hensler et al. (2010) Regulation of cortical and hippocampal 5-HT(1A) receptor function by corticosterone in GR+/- mice. Psychoneuroendocrinology. 35:469
PMID: 19766402
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
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
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
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
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

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5-HT has a potential for relaxant

Name: Anonymous

Species: Rat

Assay Type: In Vivo

5-HT1A/7 receptor (8-OHDPAT)(0.1 lmol/L)

PMID: 25692021

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