Tamsulosin potently and selectively antagonizes human recombinant α 1A/1D-adrenoceptors: Slow dissociation from the α 1A-adrenoceptor May account for selectivity for α 1A-adrenoceptor over α 1B-adrenoceptor subtype

Biological and Pharmaceutical Bulletin

Volumn 35, Issue 1, 2012, Pages 72-77

  Sato, Shuichi ^a   Hatanaka, Toshiki ^a   Yuyama, Hironori ^a   Ukai, Masashi ^a   Noguchi, Yukiko ^a   Ohtake, Akiyoshi ^a   Taguchi, Katsunari ^a   Sasamata, Masao ^a   Miyataa, Keiji ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

1 adrenoceptor antagonist; 1a adrenoceptor; 3h tamsulosin; Dissociation rate

Indexed keywords

5 METHYLURAPIDIL; 8 [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] 8 AZASPIRO[4.5]DECANE 7,9 DIONE; ALFUZOSIN; ALPHA 1A ADRENERGIC RECEPTOR; ALPHA 1B ADRENERGIC RECEPTOR; ALPHA 1D ADRENERGIC RECEPTOR; NAFTOPIDIL; PRAZOSIN; RECOMBINANT PROTEIN; SILODOSIN; TAMSULOSIN; TERAZOSIN; URAPIDIL;

ARTICLE; BINDING AFFINITY; BINDING KINETICS; CELL MEMBRANE; COMPETITIVE INHIBITION; CONTROLLED STUDY; DISSOCIATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; LIGAND BINDING;

ADRENERGIC ALPHA-1 RECEPTOR ANTAGONISTS; BINDING, COMPETITIVE; HUMANS; KINETICS; MALE; PROSTATIC HYPERPLASIA; RECEPTORS, ADRENERGIC, ALPHA-1; RECOMBINANT PROTEINS; SULFONAMIDES;

EID: 84855666968     PISSN: 09186158     EISSN: 13475215     Source Type: Journal    
DOI: 10.1248/bpb.35.72     Document Type: Article

References (28)

1. Caine M, Raz S, Zeigler M. Adrenergic and cholinergic receptors in the human prostate, prostatic capsule and bladder neck. Br. J. Urol., 47, 193-202 (1975).
2. Lepor H. Role of alpha-adrenergic blockers in the treatment of benign prostatic hyperplasia. Prostate Suppl., 3(S3), 75-84 (1990).
3. Auffenberg GB, Helfand BT, McVary KT. Established medical therapy for benign prostatic hyperplasia. Urol. Clin. North Am., 36, 443-459, v-vi (2009).
4. 1- adrenoceptors: consensus update. Pharmacol. Rev., 47, 267-270 (1995).
5. 1-adrenergic receptor subtypes in human prostate. J. Urol., 150, 546-551 (1993).
6. 1-adrenoceptor subtype mRNAs in human proximal urethra. Br. J. Pharmacol., 123, 1289-1293 (1998).
7. 1-adrenoceptor subtype-specific blockade. Br. J. Urol., 81 (Suppl. 1), 34-47, discussion, 64-66 (1998).
8. Sato S, Ohtake A, Matsushima H, Saitoh C, Usuda S, Miyata K. Pharmacological effect of tamsulosin in relation to dog plasma and tissue concentrations: prostatic and urethral retention possibly contributes to uroselectivity of tamsulosin. J. Pharmacol. Exp. Ther., 296, 697-703 (2001).
9. Sato S, Ohtake A, Hatanaka T, Suzuki M, Matsushima H, Sasamata M, Miyata K. Relationship between the functional effect of tamsulosin and its concentration in lower urinary tract tissues in dogs. Biol. Pharm. Bull., 30, 481-486 (2007).
10. 1- adrenoceptors in human prostates. J. Urol., 146, 877-880 (1991).
11. 1-adrenoceptors in human prostates with benign prostatic hypertrophy. Urol. Res., 22, 273-278 (1994).
12. 3H]prazosin binding and contraction experiments. Eur. J. Pharmacol. (Mol. Pharmacol. Sect.), 246, 275-281 (1993).
13. 1-adrenoceptor radioligand to rat and human tissues. Eur. J. Pharmacol., 348, 287-295 (1998).
14. 1-adrenoceptors in human renal medulla. J. Cardiovasc. Pharmacol., 30, 163-168 (1997).
15. Bradford MM. A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem., 72, 248-254 (1976).
16. 3H](o- ethoxyphenoxy) ethyl]amino]propyl]-2-methoxybenzenesulfonamide HCl, a potent and selective alpha-1 adrenoceptor radioligand. J. Pharmacol. Exp. Ther., 263, 201-206 (1992).
17. Taguchi K, Saitoh M, Sato S, Asano M, Michel MC. Effects of tamsulosin metabolites at alpha-1 adrenoceptor subtypes. J. Pharmacol. Exp. Ther., 280, 1-5 (1997).
18. 1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol., 22, 3099-3108 (1973).
19. 1-adrenoceptor antagonist in the lower urinary tract. Br. J. Pharmacol., 109, 1282-1289 (1993).
20. 1-adrenoceptor subtypes in prostate and prostatic urethra of rat, rabbit, dog and man. Eur. J. Pharmacol., 249, 307-315 (1993).
21. Saussy DL Jr., Goetz AS, Queen KL, King HK, Lutz MW, Rimele TJ. Structure activity relationships of a series of buspirone analogs at alpha-1 adrenoceptors: further evidence that rat aorta alpha-1 adrenoceptors are of the alpha-1D-subtype. J. Pharmacol. Exp. Ther., 278, 136-144 (1996).
22. 1-adrenoceptor antagonist, KMD-3213, and its suitability as a tritiated radioligand. Br. J. Pharmacol., 127, 19-26 (1999).
23. 1-adrenoceptors. Jpn. J. Pharmacol., 79, 447-454 (1999).
24. 3H]prazosin and [3H]tamsulosin. Eur. J. Pharmacol., 342, 85-92 (1998).
25. Motulsky HJ, Mahan LC. The kinetics of competitive radioligand binding predicted by the law of mass action. Mol. Pharmacol., 25, 1-9 (1984).
26. Korstanje C, Krauwinkel W, van Doesum-Wolters FL. Tamsulosin shows a higher unbound drug fraction in human prostate than in plasma: a basis for uroselectivity? Br. J. Clin. Pharmacol., 72, 218-225 (2011).
27. 1-acid glycoprotein and possibility of binding interactions. Eur. J. Clin. Pharmacol., 55, 437-443 (1999).
28. 1-adrenoceptor antagonist binding in human prostate and aorta. Clin. Exp. Pharmacol. Physiol., 21, 405-411 (1994).