Synonym
Tiodazosin HCl; BL-5111A; BL5111A; BL 5111A; Tiodazosin; BL-5111; BL5111; BL 5111
IUPAC/Chemical Name
(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(5-(methylthio)-1,3,4-oxadiazol-2-yl)methanone hydrochloride
InChi Key
QASXNJVDTVWTBK-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H21N7O4S.ClH/c1-27-12-8-10-11(9-13(12)28-2)20-17(21-14(10)19)25-6-4-24(5-7-25)16(26)15-22-23-18(29-15)30-3;/h8-9H,4-7H2,1-3H3,(H2,19,20,21);1H
SMILES Code
Cl.COC1=CC2=NC(=NC(N)=C2C=C1OC)N3CCN(CC3)C(=O)C4=NN=C(O4)SC
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
467.93
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Chiang J, Hermodsson G, Oie S. The effect of alpha 1-acid glycoprotein on the pharmacological activity of alpha 1-adrenergic antagonists in rabbit aortic strips. J Pharm Pharmacol. 1991 Aug;43(8):540-7. doi: 10.1111/j.2042-7158.1991.tb03533.x. PMID: 1681068.
2: Oie S, Chiang J. Alteration in the pharmacologic activity of alpha 1 adrenergic antagonists by alpha-1-acid glycoprotein. Prog Clin Biol Res. 1989;300:235-8. PMID: 2571163.
3: Forgue ST, Van Harken DR, Smyth RD. Determination of tiodazosin concentrations in human plasma with a fluorescence high-performance liquid chromatographic method. J Chromatogr. 1985 Jul 12;342(1):221-7. doi: 10.1016/s0378-4347(00)84508-9. PMID: 4044753.
4: Sznajderman M. Nowe leki hipotensyjne [New hypotensive drugs]. Pol Tyg Lek. 1984 Dec 17-31;39(51-52):1695-700. Polish. PMID: 6097887.
5: Bond RF, Johnson G 3rd. Cardiovascular adrenoreceptor function during compensatory and decompensatory hemorrhagic shock. Circ Shock. 1984;12(1):9-24. PMID: 6323052.
6: Prosser BC, Floor BJ, Klein AE, Muhammad N. Determinations of tiodazosin and levulinic acid from tablets by high-performance liquid chromatography. J Pharm Sci. 1983 Oct;72(10):1168-70. doi: 10.1002/jps.2600721015. PMID: 6644565.
7: Downing OA, Wilson KA, Wilson VG. Non-competitive antagonism of the alpha- adrenoceptor-mediated fast component of contraction of rat aorta, by doxazosin and prazosin. Br J Pharmacol. 1983 Oct;80(2):315-22. doi: 10.1111/j.1476-5381.1983.tb10036.x. PMID: 6140057; PMCID: PMC2045031.
8: Vardan S, Smulyan H, Mookherjee S, Eich R. Effects of tiodazosin, a new antihypertensive, hemodynamics and clinical variables. Clin Pharmacol Ther. 1983 Sep;34(3):290-6. doi: 10.1038/clpt.1983.170. PMID: 6883905.
9: Baughman RA Jr, Mico BA, Benet LZ. The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride. Drug Metab Dispos. 1983 Mar-Apr;11(2):143-6. PMID: 6133719.
10: Mico BA, Baughman RA Jr, Benet LZ. Determination of tiodazosin in plasma and whole blood by high-performance liquid chromatography. J Chromatogr. 1982 Jun 11;230(1):203-6. doi: 10.1016/s0378-4347(00)81451-6. PMID: 7107763.
11: Rusch NJ, De Mey JG, Vanhoutte PM. Effect of BL-5111-A, prazosin and phentolamine on responses of canine cutaneous veins to adrenergic activation. Arch Int Pharmacodyn Ther. 1980 Apr;244(2):341-3. PMID: 7406593.
12: Oates HF, Stoker LM, Stokes GS. Profile of a new prazosin congener, BL-5111A. Studies in the rat. Clin Exp Pharmacol Physiol. 1980 Jan-Feb;7(1):1-9. doi: 10.1111/j.1440-1681.1979.tb00725.x. PMID: 7379338.
13: Cohen ML, Wiley KS, Landry AS. In vitro comparison of the pre- and postsynaptic alpha adrenergic receptor blocking properties of prazosin and tiodazosin (BL5111). Clin Exp Hypertens. 1980;2(6):1067-82. doi: 10.3109/10641968009037161. PMID: 6108842.
14: Buyniski JP, Pircio AW, Schurig JE, Campbell JA. Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat. Clin Exp Hypertens. 1980;2(6):1039-66. doi: 10.3109/10641968009037160. PMID: 6108841.
15: Roebel LE, Florczyk AP, Buyniski JP. Comparative first dose effects of prazosin and tiodazosin (BL-5111) in spontaneously hypertensive rats. Res Commun Chem Pathol Pharmacol. 1979 Jan;23(1):29-35. PMID: 441514.
