Prazosin-d8

Prazosin-d8 is intended for use as an internal standard for the quantification of prazosin (Cay-15023) by GC- or LC-MS. 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 alpha2B-AR-expressing NG108 cells, respectively). It also binds to melatonin receptor 3 (MT3) in hamster brain membranes (IC50 = 7.8 nM). Prazosin inhibits peripheral and central postsynaptic alpha1-ARs with IC50 values of 0.2 and 1.7 nM in isolated dog aorta and rat brain, respectively. It decreases diastolic blood pressure in normal, renal hypertensive, and spontaneously hypertensive rats when administered at a dose of 1 mg/kg. Prazosin (1.5 mg/kg) increases the number of entries and percentage of time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, in alcohol-consuming rats and also reduces alcohol intake and alcohol-seeking behavior in alcohol-preferring rats.Formal Name: [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl-2,2,3,3,5,5,6,6-d8]-2-furanyl-methanone. CAS Number: 1006717-55-0. Molecular Formula: C19H13D8N5O4. Formula Weight: 391.5. Purity: >99% deuterated forms (d1-d8). Formulation: (Request formulation change), A solid. Solubility: Chloroform: soluble, Methanol: sparingly soluble. SMILES: COC(C(OC)=C1)=CC2=C1C(N)=NC(N3C([2H])([2H])C([2H])([2H])N(C(C4=CC=CO4)=O)C([2H])([2H])C3([2H])[2H])=N2. InChi Code: InChI=1S/C19H21N5O4/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14/h3-4,9-11H,5-8H2,1-2H3,(H2,20,21,22)/i5D2,6D2,7D2,8D2. InChi Key: IENZQIKPVFGBNW-YEBVBAJPSA-N.