70 products were found matching "K04139"!

Adrenoceptors are 7-transmembrane receptors which mediate the central and peripheral actions of the neurotransmitter, noradrenaline (norepinephrine), and the hormone and neurotransmitter, adrenaline (epinephrine). Based on both pharmacological and molecular evidence, they are divided into three major types - alpha1,...

It is an alpha2-adrenergic agonist useful in the management of opioid drawer.

Spiroxatrine is an antagonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 3 nM) and alpha2-adrenergic receptors (alpha2-ARs, Kis = 28, 1. and 1. nM for alpha2A, alpha2B, and alpha2C, respectively). It is selective for these receptors over 5-HT1D (Ki = 2 µM) and 5-HT1B at 10 µM. Spiroxatrine also induces...

Idazoxan is an antagonist of alpha2-adrenergic receptors (alpha2-ARs) and imidazoline I1 and I2 receptors (IC50s = 69, 66, and 61 nM, respectively). It selectively binds to alpha2A- and alpha2C-ARs over alpha2B-ARs (Kds = 67, 69, and 407 nM, respectively), as well as alpha2-ARs over alpha1-ARs (IC50s = 0. and 4,000...

Solulibility: DMSO: Sparingly Soluble: 1-10 mg/ml: Ethanol: Sparingly Soluble: 1-10 mg/ml.

Levonordefrin is the (-)-enantiomer of nordefrin, a synthetic derivative of norepinephrine (Cay-16673), that acts as a vasoconstrictor. Levonordefrin (1-5 µg/kg) rapidly increases blood pressure and heart rate in anesthetized dogs and has a more potent effect on blood pressure than the dextronordefrin enantiomer. It...

Medetomidine is an agonist of alpha2-adrenergic receptors (alpha2-ARs, Ki = 1.08 nM). It is selective for alpha2-ARs over alpha1-ARs (Ki = 1,750 nM). Medetomidine induces sedation in dogs. Formulations containing medetomidine have been used as sedatives in veterinary medicine. This product is also available as an...

Yohimbine is a natural alkaloid that has highest affinity for alpha2-adrenergic receptors (pKis = 8.2, 8.7, and 9.6 for human alpha2A, alpha2B, and alpha2C, respectively), with antagonist activity at these receptors. It less potently antagonizes serotonin 5-HT1 receptors (pKis = 7.3, 6.8, and 7.6 for human HT1A,...

Moxonidine is an imidazoline 1 (I1) receptor agonist (Ki = 56 nM in a radioligand binding assay). It is also an agonist of the alpha2A-adrenergic receptor (alpha2A-AR, Ki = 150 nM in a radioligand binding assay). It is selective for I1 and alpha2A-AR receptors over alpha1-, alpha2B, and alpha2C-ARs (Kis = >30,000,...

Fendiline is an alpha2-adrenergic receptor antagonist (Kd = 2.6 µM) and an L-type calcium channel blocker (IC50 = 17 µM) well-known for its coronary vasodilator effects. Fendiline has recently been reported to inhibit K-Ras plasma membrane localization (IC50 = 9.64 µM), which prevents K-Ras signal transduction and...

Rilmenidine is an antihypertensive agent. It binds to imidazole receptors in bovine rostral ventrolateral medulla homogenates (Ki = 6.1 nM), as well as alpha2-adrenergic receptors in bovine prefrontal cortex homogenates (Ki = 87 nM). Rilmenidine induces hypotension and bradycardia in anesthetized rats (ED50s = 0.25...

Xylazine is an agonist of alpha2-adrenergic receptors (Ki = 194 nM). It is an analog of clonidine, an alpha2-adrenergic receptor agonist used to reduce blood pressure. Xylazine is used for sedation, anesthesia, and analgesia in non-human mammals. This product is also available as an analytical reference standard...