Summary: An adrenergic beta-agonist used as a bronchodilator agent in asthma therapy.

Top Publications

  1. Kokubu H. [Comparison of the bronchodilating effects of five beta-adrenergic stimulants administered by inhalation to patients with bronchial asthma]. Arerugi. 1993;42:699-705 pubmed
    ..Procaterol, however, showed a more prolonged effect than salbutamol, although the initial bronchodilation was less remarkable...
  2. Comer B, Young A, Gal T. Impact of endoscopic surgical techniques on efficiency in pituitary surgery. Otolaryngol Head Neck Surg. 2011;145:732-6 pubmed publisher
    ..Despite this, a noteworthy reduction in operative times, operating room times, and room setup times is observed. The impact of endoscopic techniques on efficiency in pituitary surgery is discussed. ..
  3. Nishi H, Fukuyama T, Matsuo M, Terabe S. Chiral separation of diltiazem, trimetoquinol and related compounds by micellar electrokinetic chromatography with bile salts. J Chromatogr. 1990;515:233-43 pubmed
    ..Application to the optical purity testing of trimetoquinol hydrochloride by the area percentage method is described. A possible chiral separation mechanism is briefly mentioned. ..
  4. Danchev N, Staneva Stoytcheva D, Loukova S. Effect of beta-adrenergic and serotoninergic agents on the stress-induced behaviour of "learned helplessness" in rats. Acta Physiol Pharmacol Bulg. 1989;15:17-24 pubmed
    ..The experimental results show a favourable effect on the behavioural deficit, caused by the blocking of the adrenergic transmitter system and by increasing the activity of the serotoninergic system. ..
  5. Wu X, Li Z, Yao M, Wang H, Qu S, Chen X, et al. Identification and characterization of a novel peptide ligand of Tie2 for targeting gene therapy. Acta Biochim Biophys Sin (Shanghai). 2008;40:217-25 pubmed
    ..The difference in tumor volume between the experiment and control groups was significant (P<0.05). Our results showed that GA5 is a potentially efficient targeting element for cancer gene or molecular therapy. ..
  6. Nikulin V, Rakov I, De Los Angeles J, Mehta R, Boyd L, Feller D, et al. 1-Benzyl-1,2,3,4-tetrahydroisoquinoline-6,7-diols as novel affinity and photoaffinity probes for beta-adrenoceptor subtypes. Bioorg Med Chem. 2006;14:1684-97 pubmed
    ..Washout experiments on Chinese hamster ovary (CHO) cells expressing hu beta2-AR were helpful in identifying the isothiocyanate 18 and the azide 24 as very effective affinity and photoaffinity labels at this receptor subtype. ..
  7. Shams G, Fedyna J, Romstedt K, Adejare A, Miller D, Roche V, et al. Pharmacological properties of novel bicyclic isoquinoline analogs in isolated guinea pig atria, trachea and in human platelets: relationship to trimetoquinol. Gen Pharmacol. 1991;22:1155-63 pubmed
    ..5. These chemically novel lipophilic bicyclic compounds provide a new lead to the development of agents useful for the treatment of asthma and thrombotic disorders. ..
  8. Lezama E, Konkar A, Salazar Bookaman M, Miller D, Feller D. Pharmacological study of atypical beta-adrenoceptors in rat esophageal smooth muscle. Eur J Pharmacol. 1996;308:69-80 pubmed
    ..Trimetoquinol was as potent as (-)- isoprenaline and BRL 37344, and was the most stereoselective agonist evaluated in this tissue system. ..
  9. Markovich K, Tantishaiyakul V, Hamada A, Miller D, Romstedt K, Shams G, et al. Synthesis of halogenated trimetoquinol derivatives and evaluation of their beta-agonist and thromboxane A2 (TXA2) antagonist activities. J Med Chem. 1992;35:466-79 pubmed
    ..In contrast to platelets, (S)-(+)-8-fluoro-TMQ was an agonist in rat aorta whereas (R)-(-)-8-fluoro-TMQ was an antagonist. ..

More Information


  1. Christoff J, Bradley L, Miller D, Lei L, Rodriguez F, Fraundorfer P, et al. Synthesis and evaluation of trimetoquinol derivatives: novel thromboxane A2/prostaglandin H2 antagonists with diminished beta-adrenergic agonist activity. J Med Chem. 1997;40:85-91 pubmed
  2. Mehta R, Salazar Bookaman M, Fertel R, De Los Angeles J, Nikulin V, Fraundorfer P, et al. Biochemical and functional characterization of 1-benzyl substituted trimetoquinol affinity analogs on rat and human beta-adrenoceptors. Biochem Pharmacol. 2000;59:517-29 pubmed
    ..Thus, the lipophilic 1-benzyl ring of TMQ analogs interacts with a hydrophobic region of the beta-AR that may represent an exo-site or an allosteric binding site. ..
  3. Mashiba K, Kojima T, Ootsuka T, Kusaba T. [Yersinia psuedotuberculosis septicemia in a healthy young woman]. Kansenshogaku Zasshi. 2008;82:86-9 pubmed
    ..Y. psuedotuberculosis septicemia was diagnosed as Y. psuedotuberculosis isolated from blood and elevated serum antibody titer against Y. psuedotuberculosis 4b detected at 1:160. ..
  4. Shaheen P, Legrand S, Walsh D, Estfan B, Davis M, Lagman R, et al. Errors in opioid prescribing: a prospective survey in cancer pain. J Pain Symptom Manage. 2010;39:702-11 pubmed publisher
    ..Opioid prescribing errors were common. Females may be at greater risk of multiple errors. A PM consultation program is effective in identifying and correcting a wide variety of opioid prescribing errors. ..
  5. Camargo F, Robinson N, Berney C, Eberhart S, Baker S, DeTolve P, et al. Intravenous and intratracheal administration of trimetoquinol, a fast-acting short-lived bronchodilator in horses with 'heaves'. Equine Vet J. 2006;38:563-9 pubmed
    ..However, other routes, such as aerosol and oral, may prove useful and safe for the alleviation of bronchoconstriction typical of 'heaves'. ..
  6. Stolba U, Krebs I, Lamar P, Aggermann T, Gruber D, Binder S. Long term results after transpupillary thermotherapy in eyes with occult choroidal neovascularisation associated with age related macular degeneration: a prospective trial. Br J Ophthalmol. 2006;90:158-61 pubmed
    ..056). Although in the majority of patients far and near distance acuity could be stabilised on average a significant decrease over time after TTT was observed. Statistical comparison of months 12 and 24 showed no further deterioration. ..
  7. Franco P, Filippi A, Ricca I, Raucci C, Ricardi U. Eyelid localization in mantle cell lymphoma: long-lasting complete remission after surface brachytherapy. Tumori. 2009;95:385-8 pubmed
    ..We here report on a patient with indolent mantle cell lymphoma presenting at relapse with an isolated eyelid mass that was treated with lens-sparing surface brachytherapy resulting in durable locoregional complete remission. ..
  8. Lin C, Yang C, Chen C, Ko F, Teng C. Pharmacological characteristics of BDTI, a new isoquinoline-derived beta 2-adrenoceptor agonist, in canine trachea and rat heart. Pharmacology. 1996;53:19-27 pubmed
    ..5 and 5.7 +/- 0.6 mumol/l, respectively). The selectivity of BDTI and salbutamol for beta 2-adrenoceptors on the cAMP response were 12.4 and 14.3 times, respectively. It is concluded that BDTI is a beta 2-selective adrenoceptor agonist. ..
  9. Richards D, Davis D, Yan P, Guha S. Unusual case of small cell gastric carcinoma: case report and literature review. Dig Dis Sci. 2011;56:951-7 pubmed publisher
  10. Yabana H, Murata S, Narita H, Shimizu R, Miyagishima T, Takeda M, et al. Selective beta 1-adrenoceptor agonist activity of denopamine and its derivatives in dogs. Biol Pharm Bull. 1993;16:471-4 pubmed
    ..In this group of compounds, beta-hydroxy moiety was suggested to be requisite to potent beta-adrenoceptor stimulating action and 3,4-dimethoxyphenethyl structure was important for manifestation of beta 1-adrenoceptor selectivity. ..
  11. Shams G, Romstedt K, Lust L, Clark M, Miller D, Feller D. Beta-adrenergic receptor and platelet inhibitory activities of a new series of trimetoquinol and related benzazepine analogs. Gen Pharmacol. 1997;28:323-30 pubmed
    ..4. The selective blockade of this pathway by these compounds suggests that they may represent a new and novel class of antiplatelet drugs. ..
  12. Corrias A, Rossi G, Corona G, Corda R. [Beta 2 stimulants in the therapy of childhood asthma]. Pediatr Med Chir. 1987;9:577-9 pubmed
    ..In the older child the most important cause is determined by the reactive spasm of bronchial smooth muscle...
  13. Ahn C, Wallace L, Miller D, Feller D. Use of [3H]trimetoquinol as a radioligand in human platelets: interaction with putative endoperoxide/thromboxane A2 receptor sites. Thromb Res. 1988;50:387-99 pubmed
    ..Our studies indicate that [3H]TMQ interacts with specific binding sites with characteristics indicative of putative endoperoxide/thromboxane A2 receptors in human platelets. ..
  14. Romstedt K, Shin Y, Shams G, Doyle K, Tantishaiyakul V, Clark M, et al. Halogen-substituted trimetoquinol analogs as thromboxane A2 receptor antagonists in platelets and aorta. Biochem Pharmacol. 1993;46:2051-9 pubmed
  15. Whiting D, Tomycz N, Bailes J, De Jonge L, Lecoultre V, Wilent B, et al. Lateral hypothalamic area deep brain stimulation for refractory obesity: a pilot study with preliminary data on safety, body weight, and energy metabolism. J Neurosurg. 2013;119:56-63 pubmed publisher
    ..A larger follow-up study focused on efficacy along with a more rigorous metabolic analysis is planned to further explore the benefits and therapeutic mechanism behind this investigational therapy. ..
  16. Kretschmer L, Pratsch A. Leg swelling after inguinal sentinel lymph node biopsy and primary melanoma excision with a safety margin. J Dtsch Dermatol Ges. 2012;10:733-9 pubmed publisher
    ..More than two-thirds of patients did not have any swelling. Obesity, location of the primary melanoma at a distal site on the leg, a wide safety margin, and seromas are associated with postoperative leg swelling. ..
  17. Shams G, Wallace L, Miller D, Feller D. Effects of thromboxane A2 on thoracic aorta of young and old rats: use of selective thromboxane receptor antagonists. Pharmacology. 1990;40:27-32 pubmed
    ..09 and 5.83, respectively) and old (9.41 and 6.10, respectively) rats. We conclude that the reactivity and population of TXA2 receptors in rat vascular smooth muscle are unaffected by the aging process. ..
  18. Ahn C, Romstedt K, Wallace L, Miller D, Feller D. Characterization of the inhibition of U46619-mediated human platelet activation by the trimetoquinol isomers. Evidence for endoperoxide/thromboxane A2 receptor blockade. Biochem Pharmacol. 1988;37:3023-33 pubmed
    ..R(+)-TMQ acted as a pharmacologically selective and highly stereospecific [R(+)-TMQ much greater than S(-)-TMQ] antagonist of endoperoxide/thromboxane A2 receptor sites in platelets.(ABSTRACT TRUNCATED AT 400 WORDS) ..
  19. Kawai H, Kotake Y, Ohta S. Dopamine transporter and catechol-O-methyltransferase activities are required for the toxicity of 1-(3',4'-dihydroxybenzyl)-1,2,3, 4-tetrahydroisoquinoline. Chem Res Toxicol. 2000;13:1294-301 pubmed
    ..Thus, we consider that 1 is taken up into dopaminergic neurons via the dopamine transporter and then converted by COMT to 5, which has cytotoxic and parkinsonism-inducing activities. ..
  20. Markov M, Ivanov C, Uzunov P, Ovcharov R. Effects of compound IS-35 on intraocular pressure. Methods Find Exp Clin Pharmacol. 1988;10:449-52 pubmed
    ..The experimental study on the beta-adrenergic adenylate cyclase showed that the mechanism of action of IS-35 on ophthalmotonus most probably is similar to the effect of timolol and is due to the suppression of aqueous humor formation. ..
  21. Kumar R, Singh P. Quantitative structure-activity relationship study of iodinated analogues of trimetoquinol as highly potent beta 2-adrenoceptor ligands. Indian J Biochem Biophys. 1998;35:390-2 pubmed
  22. Harrold M, Gerhardt M, Romstedt K, Feller D, Miller D. Synthesis and platelet antiaggregatory activity of trimetoquinol analogs as endoperoxide/thromboxane A2 antagonists. Drug Des Deliv. 1987;1:193-207 pubmed
  23. Nishi H, Nakamura K, Nakai H, Sato T, Terabe S. Enantiomeric separation of drugs by affinity electrokinetic chromatography using dextran sulfate. Electrophoresis. 1994;15:1335-40 pubmed
    ..The choice of pH and the concentration of dextran sulfate has been important for the improvement in selectivity. ..
  24. Shin Y, Romstedt K, Miller D, Feller D. Interactions of nonprostanoid trimetoquinol analogs with thromboxane A2/prostaglandin H2 receptors in human platelets, rat vascular endothelial cells and rat vascular smooth muscle cells. J Pharmacol Exp Ther. 1993;267:1017-23 pubmed
  25. de los Angeles J, Nikulin V, Shams G, Konkar A, Mehta R, Feller D, et al. Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands. J Med Chem. 1996;39:3701-11 pubmed
    ..Thus, manipulation of the 1-benzyl moiety of trimetoquinol (1) has resulted in analogs that exhibit potent beta 2-AR binding affinity and significantly lower beta 1-AR and TP receptor affinities. ..
  26. Nishi H. Enantiomer separation of basic drugs by capillary electrophoresis using ionic and neutral polysaccharides as chiral selectors. J Chromatogr A. 1996;735:345-51 pubmed
    ..A brief mechanism of enantiorecognition by polysaccharides is also described. ..
  27. Nelson M, Lanza L, Reeder C, Scott R, McCullough A, Chandrasekaran K, et al. Histologic remission of cardiac amyloidosis: a case report. Amyloid. 2012;19:106-9 pubmed publisher
    ..This observation suggests a mechanism of treatment response and that with appropriately timed treatment, cardiac deposition of amyloid fibrils can be completely reversed. ..
  28. Sugihara J, Furuuchi S, Nakano K, Harigaya S. Studies on intestinal lymphatic absorption of drugs. I. Lymphatic absorption of alkyl ester derivatives and alpha-monoglyceride derivatives of drugs. J Pharmacobiodyn. 1988;11:369-76 pubmed
    ..It was concluded that alpha-monoglyceride derivatives of drugs were absorbed via the lymphatic system and transported into blood, yielding the parent drug in blood. ..
  29. Shams G, Harrold M, Grazyl B, Miller D, Feller D. Pharmacological evaluation of the beta-adrenoceptor agonist properties of N-benzyl substituted trimetoquinol analogues. Eur J Pharmacol. 1990;184:251-6 pubmed
    ..The results show that varying the nature of substituents on the N-benzyl ring of TMQ produces compounds which retain greater beta 2-selectivity. ..
  30. Konkar A, Fraundorfer P, Fertel R, Burkman A, Miller D, Feller D. Pharmacological activities of trimetoquinol and 1-benzyl halogen-substituted analogues on rat beta-adrenoceptor subtypes. Eur J Pharmacol. 1996;305:63-71 pubmed
    ..These results suggest that 3',5'-diiodotrimetoquinol is a promising drug for further chemical modification in the development of selective beta 3-adrenoceptor ligands. ..
  31. Fraundorfer P, Fertel R, Miller D, Feller D. Biochemical and pharmacological characterization of high-affinity trimetoquinol analogs on guinea pig and human beta adrenergic receptor subtypes: evidence for partial agonism. J Pharmacol Exp Ther. 1994;270:665-74 pubmed
    ..Thus, TMQ and halogenated TMQ derivatives bind stereoselectively to beta-AR with high affinity, and may be classified as partial beta-AR agonists. ..
  32. Kawai H, Makino Y, Hirobe M, Ohta S. Novel endogenous 1,2,3,4-tetrahydroisoquinoline derivatives: uptake by dopamine transporter and activity to induce parkinsonism. J Neurochem. 1998;70:745-51 pubmed
    ..2 pmol/min/mg of protein, respectively. Thus, endogenous 3',4'DHBnTIQ may be actively transported into dopaminergic neurons and accumulated there, contributing at least in part to the induction of idiopathic Parkinson's disease. ..
  33. Bureau M, De Clerck F, Lefort J, Arreto C, Vargaftig B. Thromboxane A2 accounts for bronchoconstriction but not for platelet sequestration and microvascular albumin exchanges induced by fMLP in the guinea pig lung. J Pharmacol Exp Ther. 1992;260:832-40 pubmed
  34. Camargo F, Robinson N, Dirikolu L, Berney C, Eberhart S, Derksen F, et al. Plasma and urinary concentrations of trimetoquinol by LC-MS-MS following intravenous and intra-tracheal administration to horses with heaves. J Vet Pharmacol Ther. 2008;31:501-10 pubmed publisher
    ..We report that the ELISA kit was unable to detect TMQ from any of the samples generated in these studies. ..
  35. Yamashita K, Shimizu K. Endoscopic video-assisted breast surgery: procedures and short-term results. J Nippon Med Sch. 2006;73:193-202 pubmed
    ..The original shapes of the breast were preserved. All patients expressed their great satisfaction with VABS. VABS can be considered as a surgical option and can provide aesthetic advantages for patients with breast disease. ..
  36. de Beer J, Petruccelli D, Zalzal P, Winemaker M. Single-incision, minimally invasive total hip arthroplasty: length doesn't matter. J Arthroplasty. 2004;19:945-50 pubmed
    ..The mini-exposure creates technical challenges that have the potential to adversely affect primary THA outcome. ..
  37. Okamura S, Oshimoto H, Sakamoto T, Kusano M, Sekiguchi T, Mori M. Beta-adrenoreceptor agonists for diffuse esophageal spasm. J Gastroenterol. 2002;37:229-30 pubmed
  38. Konkar A, Vansal S, Shams G, Fraundorfer P, Zheng W, Nikulin V, et al. Beta-adrenoceptor subtype activities of trimetoquinol derivatives: biochemical studies on human beta-adrenoceptors expressed in chinese hamster ovary cells. J Pharmacol Exp Ther. 1999;291:875-83 pubmed
    ..Our results indicate that 6, 7-dihydroxy-catechol-modified and 1-benzyl halogen-substituted derivatives of TMQ represent promising leads for the development of beta(3)-adrenoceptor-selective agonists. ..
  39. Camargo F, Robinson N, Berney C, Eberhart S, Baker S, DeTolve P, et al. Trimetoquinol: bronchodilator effects in horses with heaves following aerosolised and oral administration. Equine Vet J. 2007;39:215-20 pubmed
    ..Oral TMQ was therapeutically ineffective. Aerosol administration of TMQ is a safe and effective method of producing bronchodilation in horses. ..
  40. Khoury J, Saluja R, Goldman M. The effect of botulinum toxin type A on full-face intense pulsed light treatment: a randomized, double-blind, split-face study. Dermatol Surg. 2008;34:1062-9 pubmed publisher
    ..Other efficacy measures showed comparable improvements with both regimens. The adjunctive use of BTX enhances the improvement in small wrinkles and fine lines, and possibly erythema, achieved with IPL alone. ..
  41. Fraundorfer P, Lezama E, Salazar Bookaman M, Fertel R, Miller D, Feller D. Isomeric-activity ratios of trimetoquinol enantiomers on beta-adrenergic receptor subtypes: functional and biochemical studies. Chirality. 1994;6:76-85 pubmed
  42. Shams G, Romstedt K, Gerhardt M, Harrold M, Miller D, Feller D. Pharmacological evaluation of the beta-adrenoceptor agonist and thromboxane receptor blocking properties of 1-benzyl substituted trimetoquinol analogues. Eur J Pharmacol. 1990;184:21-31 pubmed
  43. Shin Y, Romstedt K, Doyle K, Harrold M, Gerhardt M, Miller D, et al. Pharmacologic antagonism of thromboxane A2 receptors by trimetoquinol analogs in vitro and in vivo. Chirality. 1991;3:112-7 pubmed
    ..On the other hand, (-)-(S)-TMQ did not protect animals against death. Protection of U46619-induced cardiopulmonary thrombosis by TMQ analogs was seen at doses of 3-100 mg/kg.(ABSTRACT TRUNCATED AT 250 WORDS) ..
  44. Dainese L, Guarino A, Burba I, Esposito G, Pompilio G, Polvani G, et al. Heart valve engineering: decellularized aortic homograft seeded with human cardiac stromal cells. J Heart Valve Dis. 2012;21:125-34 pubmed
    ..Hence, CStCs appear to be a potentially useful cell type for engineered heart valves. ..
  45. Konkar A, Nikulin V, De Los Angeles J, Hong S, Fertel R, Miller D, et al. Biochemical activities of trimetoquinol analogs at human beta(1)- and beta(3)-adrenergic receptors. Pharmacology. 2001;62:45-55 pubmed