Losulazine

SKU: orb1819161

Description

Losulazine is a novel antihypertensive agent whose mechanism, while not fully elucidated, requires a functional sympathetic nervous system for activity. It serves as a research tool for studying sympathetic modulation in hypertension, applicable in both in vivo animal models and in vitro receptor interaction assays.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 72141-57-2
• MW: 558.55
• Purity: 98.94%
• Formula: C₂₇H₂₂F₄N₄O₃S
• SMILES: N(C=1C2=C(C=C(C(F)(F)F)C=C2)N=CC1)C3=CC=C(C(=O)N4CCN(S(=O)(=O)C5=CC=C(F)C=C5)CC4)C=C3
• Target: Norepinephrine,Others,Dopamine Receptor
• Solubility: DMSO:7.31 mg/mL (13.09 mM)

Bioactivity

• In Vivo:
  Groups of six female Upjohn Sprague-Dawley rats were treated orally with 10 mg/kg/day of losulazine and/or 18.75 mg/kg/day of bromocriptine for 15 or 27 days. Six rats were treated with losulazine plus 6.25 mg/kg/day of bromocriptine for 16 days followed by losulazine alone for 11 days. Rats treated with losulazine only were depleted of hypothalamic catecholamines, were hyperprolactinemic, and had interrupted estrous cycles and attenuated vaginal mucosa. Treatment with bromocriptine, a dopamine receptor agonist, resulted in suppression of serum prolactin and normal estrous cycles. Rats reverted back to hyperprolactinemia and anestrus shortly after bromocriptine withdrawal. These results suggest that hyperprolactinemia mediated through hypothalamic dopamine depletion is the mechanism of anestrus in rats treated with losulazine.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Norepinephrine (NE), DopamineReceptor, Dopamine, Dopamine Receptor

Compound Identifiers

PubChem CID

54750