Home GPCR & G Protein Adrenergic Receptor antagonist Prazosin HCl

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Prazosin HCl Adrenergic Receptor antagonist

Cat.No.S1424

Prazosin HCl (cp-12299-1) is a competitive alpha-1 adrenoceptor antagonist, used to treat high blood pressure or benign prostatic hyperplasia.
Prazosin HCl Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 419.86

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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 3 mg/mL (7.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 419.86 Formula

C19H21N5O4·HCl

 Storage (From the date of receipt)
CAS No. 19237-84-4 Download SDF Storage of Stock Solutions

Synonyms cp-12299-1 Smiles COC1=C(C=C2C(=C1)C(=NC(=N2)N3CCN(CC3)C(=O)C4=CC=CO4)N)OC.Cl

Mechanism of Action

Targets/IC50/Ki
alpha-adrenergic receptor
In vitro
Prazosin leads to a significant increase in VEGF concentration in endothelial cells and angiogenesis only if eNOS is present. Prazosin binds to the α1-adrenergic receptors that are present on smooth muscle cells surrounding all larger blood vessels. Prazosin (0.1 nM) blocks the increases in perfusion pressure caused by electrical stimulation of the perimesenteric nerves but does not significantly reduce the vasomotor effect of exogenous noradrenaline.
In vivo
Prazosin application leads to the expansion of the capillary system by modulation of the hemodynamic environment (flow rate, shear stress) in skeletal muscle. Prazosin induces angiogenesis in extensor digitorum longus (EDL) muscles of C57BL/6 mice but not eNOS-knockout mice. Prazosin (0.5-2.0 mg/kg) blocks Yohimbine-induced reinstatement of food and alcohol seeking, as well as footshock-induced reinstatement of alcohol seeking in rats. Prazosin (0.2mg kg(-1) s.c.) causes an enhancement of a suppression of conditioned avoidance response in the presence of the dopamine D2 receptor antagonist raclopride (0.05-0.20 mg/kg s.c.) in rats. Prazosin administration alone (1 mg/kg, s.c.) only slightly reduces horizontal activity during an initial 10 min measurement period, although it consistently reduces rearing in freely moving rats. Prazosin effectively suppresses the locomotor stimulation caused by either dose of MK-801 throughout the whole observation period in freely moving rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11129112/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8864686/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05189977 Terminated
Post-traumatic Stress Disorder (PTSD)
Otsuka Pharmaceutical Development & Commercialization Inc.|Iqvia Pty Ltd
 September 7 2022 Phase 1
NCT04365257 Terminated
COVID-19
Johns Hopkins University|Fast Grants
 May 13 2020 Phase 2
NCT03045016 Completed
Acute Stress Disorder
Hospices Civils de Lyon
 April 21 2017 Phase 2
NCT02193256 Completed
Cigarette Smoking|Alcohol Use Disorders
Yale University|National Institute on Alcohol Abuse and Alcoholism (NIAAA)
 July 2014 Early Phase 1
NCT01178138 Completed
Continuous Methamphetamine Abuse
University of Arkansas|National Institute on Drug Abuse (NIDA)
 December 2009 Phase 2

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