- Differences in potency and efficacy of a series of phenylisopropylamine/phenylethylamine pairs at 5-HT(2A) and 5-HT(2C) receptors.
-
The pharmacological profile of a series of (+/-)-2,5-dimethoxy-4-(X)-phenylisopropylamines (X=I, Br, NO(2), CH(3), or H) and corresponding phenylethylamines, was determined in Xenopus laevis oocytes injected with cRNA coding for rat 5-HT(2A) or 5-HT(2C) receptors. The efficacy and relative potency of these drugs were determined and compared to classical 5-HT(2) receptor agonists and antagonists. The rank order of agonist potency at the 5-HT(2A) receptor was: alpha-methyl-5-HT=5-HT>m-CPP>MK-212; at the 5-HT(2C) receptor the order was: 5-HT>alpha-methyl-5-HT>MK-212>m-CPP. All these compounds were full agonists at the 5-HT(2C) receptor, but alpha-methyl-5-HT and m-CPP showed lower efficacy at the 5-HT(2A) receptor. 4-(4-Fluorobenzoyl)-1-(4-phenylbutyl)piperidine (4F 4PP) was 200 times more potent as a 5-HT(2A) antagonist than at 5-HT(2C) receptors. Conversely, RS 102221 was 100 times more potent as a 5-HT(2C) antagonist, confirming their relative receptor selectivities. The phenylisopropylamines were partial agonists at the 5-HT(2A) receptor, with I(max) relative to 5-HT in the 22+/-7 to 58+/-15% range; the corresponding phenylethylamines had lower or undetectable efficacies. All these drugs had higher efficacies at 5-HT(2C) receptors; DOI was a full 5-HT(2C) agonist. 2C-I and the other phenylethylamines examined showed relative efficacies at the 5-HT(2C) receptor ranging from 44+/-10% to 76+/-16%. 2C-N was a 5-HT(2) receptor antagonist; the mechanism was competitive at the 5-HT(2A), but non-competitive at the 5-HT(2C) receptor. The antagonism was time-dependent at the 5-HT(2C) receptor but independent of pre-incubation time at the 5-HT(2A) receptor subtype. The alpha-methyl group determines the efficacy of these phenylalkylamines at the 5-HT(2A) and 5-HT(2C) receptors.
- Acuna-Castillo, Claudio,Villalobos, Claudio,Moya, Pablo R,Saez, Patricio,Cassels, Bruce K,Huidobro-Toro, J Pablo
-
-
Read Online
- Organic compound for detecting content of metal ions in urine, and application thereof
-
The invention discloses an organic compound for detecting the content of metal ions in urine. N, N-diacetoxyl-2,5-dialkoxyaniline is as a metal ion complex, and a chromogenic group or a fluorescence group is introduced to the molecule of the N, N-diacetox
- -
-
Paragraph 0026; 0046
(2018/08/03)
-
- Immunoassay for Phenethylamines of the 2C and DO Sub-Families
-
Immunoassay methods and their requisite components for the detection and determination of phenethylamines of the 2C and DO sub-families are described.
- -
-
-
- IMMUNOASSAY FOR COMPOUNDS OF THE NBOME FAMILY
-
An immunoassay method for detecting and determining 'NBOMe' family designer drugs is described. Also described are components for use in implementing the method, namely, antibodies, detection agents, solid state devices and kits as well as immunogens used to raise the antibodies.
- -
-
-
- Immunoassay for Phenethylamines of the 2C and DO Sub-Families
-
Immunoassay methods and their requisite components for the detection and determination of phenethylamines of the 2C and DO sub-families are described.
- -
-
-
- Multicyclic aromatic compounds and uses thereof
-
Multicyclic aromatic compounds useful as complexing agents having the general formula: Methods of complexing and quantitating a component in a sample such as urea or guanidine are also disclosed.
- -
-
-