A centrally acting antihypertensive agonist that targets I1 imidazoline receptors with a Ki value of 7.1 nM and demonstrates weaker affinity for I2 (Ki = 5.2 µM) and α2-adrenergic receptors; induces autophagy as evidenced by a dose-dependent increase of LC3-II levels in PC12 cells

Rilmenidine (hemifumarate) – 5 mg

Brand:
Cayman
CAS:
207572-68-7
Storage:
-20
UN-No:
Non-Hazardous - /

Rilmenidine is a centrally acting antihypertensive agent that has been shown to lower arterial pressure in various animal models by inhibiting the tonic activity of sympathoexcitatory neurons in the rostral ventrolateral medulla.{25847} Rilmenidine targets the nonadrenergic imidazoline-binding site I1 receptor with a Ki value of 7.1 nM and demonstrates weaker affinity for the I2 receptor with a Ki value of 5.2 µM.{25846,30142} It can also act as an agonist of α2-adrenergic receptors, but demonstrates ~30-fold greater selectivity for I1 receptors compared to α2-adrenergic receptors.{30141} Rilmenidine is reported to induce autophagy as evidenced by a ~350% increase in LC3-II levels in PC12 cells when treated with 1 µM of the I1 agonist.{30143}  

 

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Description

A centrally acting antihypertensive agonist that targets I1 imidazoline receptors with a Ki value of 7.1 nM and demonstrates weaker affinity for I2 (Ki = 5.2 µM) and α2-adrenergic receptors; induces autophagy as evidenced by a dose-dependent increase of LC3-II levels in PC12 cells

Formal name: N-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine, 2E-butenedioate (2:1)

Synonyms:  Oxaminozoline|S 3341

Molecular weight: 238.3

CAS: 207572-68-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Neuroscience

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