113 products were found matching "K04135"!

WB 4101 is an antagonist of alpha-adrenergic receptors (alpha-ARs). It inhibits norepinephrine-induced contraction of isolated rat vas deferens (pA2 = 9.8). WB 4101 also inhibits contractions induced by carbachol (carbamoylcholine, Cay-14486) in isolated guinea pig taenia caeci (pA2 = 8.9). Formal Name:...

Recombinant CHO-K1 cells stably overexpress human adrenoceptor alpha 1A (ADRA1A) on the surface and contain high levels of G protein Galphaq to couple with the receptor in downstream signaling pathways.

Urapidil-d3 is intended for use as an internal standard for the quantification of urapidil (Cay29004) by GC- or LC-MS. Urapidil is an antagonist of alpha1-adrenergic receptors (alpha1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It selectively binds to alpha1- over alpha2-ARs (IC50s =...

An oxidized derivative of epinephrine, induces dsDNA breaks in RFL-6 fibroblasts at 250 µM, increases the blood levels of fibrinogen in rats at 20 mg/kg

An atypical antipsychotic, selectively binds to sigma receptors over alpha1-ARs and dopamine D2 receptors (IC50s = 112, 520, and 6,340 nM, respectively), inhibits the conditioned avoidance response and apomorphine-induced stereotypy in rats (ED50s = 26.4 and 33 mg/kg, respectively). Formulation: A solid. InChI:...

Carvedilol is an antagonist of the beta-adrenergic receptor (beta-AR, Kds = 1.78, 0.4, and 5.01 nM for beta1-, beta2-, and beta3-ARs, respectively). It also selectively binds to alpha1- over alpha2-ARs (Kis = 0.81 and 3,400 nM, respectively). Carvedilol reverses increases in heart rate induced by the beta1-AR...

Prazosin is an antagonist of alpha1-adrenergic receptors (alpha1-ARs). It selectively binds to alpha1-ARs with Ki values of 0.2, 0.25, and 0.32 nM for the human recombinant alpha1A-, alpha1B-, and alpha1D-ARs, respectively, over alpha2-ARs (Kis = 340 and 3.7 nM in alpha2A-AR-expressing HT-29 cells and...

Ifenprodil is an antagonist of NR1A/NR2B subunit-containing NMDA receptors (IC50 = 340 nM). It is selective for NR1A/NR2B subunit-containing NMDA receptors over those containing NR1A/NR2A or NR1A/NR2C subunits (IC50s = 20 and >100 µM, respectively) but also binds to sigma 1 (sigma1) receptors, emopamil binding...

L-Phenylephrine is an adrenergic alpha1A receptor agonist (Ki = 1.4 µM) that demonstrates selectivity against the alpha1B and alpha1C receptor subtypes (Kis = 23.9 and 47.8 µM, respectively). By stimulating adrenergic alpha1 receptors, L-phenylephrine can induce aortic smooth muscle contractions, although reported...

Tolazoline is an alpha1-adrenergic receptor (alpha1-AR, IC50 = 3,200 nM) and alpha2-AR antagonist (Kis = 112, 1,230, 354, and 173 nM for alpha2A, alpha2B-, alpha2C-, and alpha2D-ARs, respectively). Tolazoline inhibits alpha-AR agonist-induced contractions in isolated human corpus cavernosum smooth muscle (IC50 = 0.1...

Cirazoline is an alpha1-adrenergic receptor (alpha1-AR) agonist (Kis = 120, 960, and 660 nM for recombinant alpha1A-, alpha1B-, and alpha1D-ARs, respectively, in CHO cell membranes). It acts as a full agonist at alpha1A- and a partial agonist at alpha1B- and alpha1D-ARs in vitro (EC50s = 70.7, 79.4, and 239.8 nM,...

Alfuzosin is a post-synaptic alpha1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH). It displays high-affinity with non-selectivity for the three known human alpha1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for alpha1A, alpha1B, and...