Asset Details
Do you wish to reserve the book?
Pharmacological evaluation of the beta-adrenoceptor subtype interactions of trimetoquinol (TMQ) and related analogs
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Pharmacological evaluation of the beta-adrenoceptor subtype interactions of trimetoquinol (TMQ) and related analogs
Do you wish to request the book?
Pharmacological evaluation of the beta-adrenoceptor subtype interactions of trimetoquinol (TMQ) and related analogs
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Dissertation
Pharmacological evaluation of the beta-adrenoceptor subtype interactions of trimetoquinol (TMQ) and related analogs
1996
Overview
Trimetoquinol belongs to a novel tetrahydroisoquinoline class of compounds, and is a non-selective highly potent agonist of $\\beta$-adrenoceptors. The pharmacological activities of trimetoquinol and analogs were evaluated in rat tissues containing predominantly $\\beta\\sb1$- and $\\beta\\sb2$-adrenoceptors, and in homogeneous populations of rat $\\beta\\sb3$-, human $\\beta\\sb1$- and $\\beta\\sb3$-adrenoceptors to determine the chemical specificity for interaction with $\\beta$-adrenoceptor subtypes. The 1-benzyl diiodinated analog of trimetoquinol exhibited selectivity for the rat $\\beta\\sb3$-adrenoceptor. Pharmacological evaluation of a series of trimetoquinol analogs modified at the 1-carbon and 6,7-dihydroxybenzyl ring on homogeneous populations of human $\\beta$-adrenoceptor subtypes revealed that: (1) the diiodinated benzyl analogs displayed high affinity for the $\\beta\\sb1$- and $\\beta\\sb3$-subtypes, and high efficacy for interactions with $\\beta\\sb3$-adrenoceptors; (2) modifications of the 4$\\sp\\prime$-position of the benzyl ring gave rise to compounds which exhibited $\\beta\\sb3$-adrenoceptor selectivity, and included 3$\\sp\\prime,5\\sp\\prime$-diiodo-4$\\sp\\prime$-amino and 3$\\sp\\prime,5\\sp\\prime$-diiodo-4$\\sp\\prime$-H substituents; and (3) bioisosteric replacement of the 6,7-dihydroxybenzyl ring of trimetoquinol with a thiazolopyridine nucleus gave compounds which were selective agonists of the $\\beta\\sb3$-adrenoceptor. Selective activation of $\\beta\\sb3$-adrenoceptors is proposed to lead to enhanced lipolysis and increase in sensitivity to insulin. Thus, several of these trimetoquinol analogs represent promising leads for the development of agents that may be useful for the treatment of obesity and non-insulin dependent diabetes.
Publisher
ProQuest Dissertations & Theses
Subject
ISBN
9780591179699, 0591179695
