Stereoconfiguration of antiallergic and immunologic drugs

L Bielory, A Leonov - Annals of Allergy, Asthma & Immunology, 2008 - Elsevier
OBJECTIVE: To review the concept of chirality and its current role in the pharmacology of
antiallergic, antiasthmatic, and immunologic agents. DATA SOURCES: Ovid MEDLINE and …

Structure-affinity relationships and stereospecificity of several homologous series of local anesthetics for the beta2-adrenergic receptor

J Butterworth, RL James, J Grimes - Anesthesia & Analgesia, 1997 - journals.lww.com
Local anesthetics inhibit binding of ligands to beta 2-adrenergic receptors (beta 2 ARs), and,
as a consequence, inhibit intracellular cAMP production. We hypothesized that among …

Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human β3-adrenoceptors

BD Popp, DS Hutchinson, BA Evans… - European journal of …, 2004 - Elsevier
This study examines the stereoselectivity profile of recombinant mouse, rat and human β3-
adrenoceptors expressed in Chinese Hamster Ovary (CHO-K1) cells using radioligand …

Pharmacological study of atypical β-adrenoceptors in rat esophageal smooth muscle

EJ Lezama, AA Konkar, M Margarita, DD Miller… - European journal of …, 1996 - Elsevier
The chemical specificity for the β-adrenoceptor mediated relaxation of rat esophageal
smooth muscle was evaluated using selective and non-selective β-adrenoceptor agonists …

1-Benzyl-1, 2, 3, 4-tetrahydroisoquinoline-6, 7-diols as novel affinity and photoaffinity probes for β-adrenoceptor subtypes

VI Nikulin, IM Rakov, E Joseph, RC Mehta… - Bioorganic & medicinal …, 2006 - Elsevier
Trimetoquinol (TMQ, 1) is a potent non-selective β-adrenoceptor (β-AR) agonist possessing
a tetrahydroisoquinoline (THI) structure. The binding site for 1-trimethoxybenzyl group of 1 …

2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines:  Novel Selective β3-Adrenoceptor Agonists

W Zheng, VI Nikulin, AA Konkar… - Journal of medicinal …, 1999 - ACS Publications
Trimetoquinol (TMQ, 7) is a potent nonselective β-adrenoceptor (AR) agonist. Replacement
of the catechol moiety of TMQ with a 2-aminothiazole group resulted in novel …

β-Adrenoceptor subtype activities of trimetoquinol derivatives: biochemical studies on human β-adrenoceptors expressed in Chinese hamster ovary cells

AA Konkar, SS Vansal, G Shams, PF Fraundorfer… - … of Pharmacology and …, 1999 - ASPET
The β-adrenoceptor activities of trimetoquinol (TMQ) isomers and selected derivatives were
evaluated on human β-adrenoceptor subtypes expressed in Chinese hamster ovary cells. In …

Synthesis and human β-adrenoceptor activity of 1-(3, 5-diiodo-4-methoxybenzyl)-1, 2, 3, 4-tetrahydroisoquinolin-6-ol derivatives in vitro

Y He, VI Nikulin, SS Vansal, DR Feller… - Journal of medicinal …, 2000 - ACS Publications
Trimetoquinol (1, TMQ) is a potent nonselective β-adrenergic receptor (AR) agonist and a
thromboxane A2/prostaglandin endoperoxide (TP) receptor antagonist, while 3 ', 5 '-diiodo …

Pharmacological activities of trimetoquinol and 1-benzyl halogen-substituted analogues on rat β-adrenoceptor subtypes

AA Konkar, PF Fraundorfer, RH Fertel… - European journal of …, 1996 - Elsevier
The β-adrenoceptor activity profile of trimetoquinol and its 1-benzyl halogen-substituted
analogues was studied in rat tissues containing primarily β1 (atria)-, β2 (trachea)-and …

[图书][B] β3 Adrenoreceptor

AD Strosberg - 2000 - books.google.com
Since the first pharmacological description of an'atypical'adrenoreceptor and the cloning of
theAR gene, research interest in this receptor has grown considerably and many advances …