3-[(4,5-Dihydro-1H-imidazol-2-ylmethyl)-p-tolyl-amino]-phenol(Phentolamine) PHENTOLAMINE Regitine 3-[(4,5-Dihydro-1H-imidazol-2-ylmethyl)-p-tolyl-amino]-phenol BDBM50008789 CHEMBL597 (Phentolamine)3-[(4,5-Dihydro-1H-imidazol-2-ylmethyl)-p-tolyl-amino]-phenol Phentolamine;3-[(4,5-Dihydro-1H-imidazol-2-ylmethyl)-p-tolyl-amino]-phenol PHENTOLAMINE3-[(4,5-Dihydro-1H-imidazol-2-ylmethyl)-p-tolyl-amino]-phenol
cid_91430 3-[N-(2-imidazolin-2-ylmethyl)-4-methyl-anilino]phenol;mesylic acid PHENTOLAMINE MESYLATE MLS000069487 PHENTOLAMINE 3-[4,5-dihydro-1H-imidazol-2-ylmethyl-(4-methylphenyl)amino]phenol;methanesulfonic acid 3-[N-(2-imidazolin-2-ylmethyl)-4-methyl-anilino]phenol;hydrochloride 3-[N-(4,5-dihydro-1H-imidazol-2-ylmethyl)-4-methylanilino]phenol;methanesulfonic acid cid_5775 SMR000059054 BDBM31046
- ChEMBL_198191 (CHEMBL799119) Inhibition of AA+phentolamine by the compound in response of SEC
- ChEMBL_198195 (CHEMBL799123) Inhibition of U-46,619 + phentolamine by the compound in response of SEC
- ChEMBL_33508 (CHEMBL647005) The compound's binding affinity against Alpha-2B adrenergic receptor from rat kidney homogenate in the presence of phentolamine
- ChEMBL_303771 (CHEMBL829301) In vitro binding affinity measured by displacement of [3H]rauwolscine from alpha-2c adrenergic receptor expressed in CHO cells in presence of phentolamine
- ChEMBL_39354 (CHEMBL654960) Beta-adrenergic agonistic activity in rat proximal colon in presence of phentolamine (10 uM), desmethylimipramine (0.5 uM) and hydrocortisone (30 uM)
- ChEMBL_1340541 (CHEMBL3254965) Agonist activity at beta-adrenergic receptor in Sprague-Dawley rat cerebral cortex assessed as [3H]cAMP accumulation by liquid scintillation spectroscopy in presence of phentolamine
- alpha-Adrenoceptor Radioligand Binding Assay The binding affinity of compound was evaluated using [3H] Clonidine as ligand in competition binding experiments. Nonspecific binding was determined as the concentration of ligand bound in the presence of 2 uM phentolamine. Ki values were determined by the equation: Ki = IC50/(1 + [clonidine]/KD).
- Receptor Binding Assay Alpha-1 receptor binding studies were performed according to the methods described by Greengrass and Bremner (Eur. J. Pharmacol., 55:323-326, 1979) on rat cortical membrane preparation using [3H]-prazosine (0.22-0.37 nM) as ligand. The non-specific binding was determined in the presence of 10 μM phentolamine.
- Alpha2-Adrenergic Receptor Binding Assay The membrane preparation was prepared as described by Newman-Tancredi, A.; Nicolas, J,-P.; Audinot, V.; Gavaudan, S.; Verriele, L.; Touzard, M.; Chaput, C.; Richard, N.; Millan, N. J. (Action of alpha2 Adrenoreceptor Ligands at alpha2A and 5-HT1A Receptors: the Antagonist, Atipamezole, and the Agonist, Dexmedetomidine, are Highly Selective for alpha2A Adrenoreceptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 1998, 358, 197-206). These membranes (30 ug proteins/ml for CHO-halpha2A and CHO-halpha2B, 100 ug protein/ml for CHO-halpha2C) were incubated for 60 min at ambient temperature in binding buffer (33 mM Tris-HCl, 1 mM EDTA, pH 7.5) in a final volume of 500 uL containing 0.8 or 1 or 2 nM [3H]RX821002 respectively for the adrenergic receptors halpha2A, halpha2B and halpha2C. Incubation was halted by rapid vacuum filtration through GF/C glass fibre filters followed by three successive washings in ice-cold binding buffer. Non-specific binding was determined using 10 uM phentolamine.
- Radioligand Binding Assay Alpha1-adrenergic Receptor: Radioligand binding was performed using tissue (rat cortex). All assays were carried out in duplicates. 50 μL working solution of the tested compounds, 50 μL [3H]-prazosin (final concentration 0.2 nM, Kd 0.2 nM) and 150 μL tissue suspension prepared in assay buffer (50 mM Tris-HCl, pH 7.6) were transferred to polypropylene 96well microplate using 96wells pipetting station Rainin Liquidator (MettlerToledo). Phentolamine (10 μM) was used to define nonspecific binding. Microplate was covered with a sealing tape, mixed and incubated for 30 minutes at 30° C. The reaction was terminated by rapid filtration through GF/B filter mate. Ten rapid washes with 200 μL 50 mM Tris-HCl buffer (4° C., pH 7.6) were performed using automated harvester system Harvester-96 MACH III FM (Tomtec). The filter mates were dried at 37° C. in forced air fan incubator and soaked in 10 mL of liquid scintillation cocktail Ultima Gold MV (PerkinElmer, USA). After even distribution of scintillation cocktail filter bag was sealed. Radioactivity was counted in MicroBeta2 scintillation counter (PerkinElmer) at approximately 30% efficiency. Data were fitted to a one-site curve-fitting equation with Prism 6 (Graph Pad Software) and Ki values were estimated from the Cheng-Prusoff equation.