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DMPX (3,7-dimethyl-1-propargylxanthine) is a caffeine analog which displays affinity to A 2 adenosine receptors, in contrast to the A 1 subtype receptors. [1] DMPX had 28× and 15× higher potency than caffeine in blocking peripheral and central NECA-responses. The locomotor stimulation caused by DMPX (ED 50 10 μmol/kg) was similarly higher ...
The concept of replacing hydrogen with deuterium is an example of bioisosterism, whereby similar biological effects to a known drug are produced in an analog designed to confer superior properties. [5] The first patent in the US granted for deuterated molecules was in the 1970s. Since then patents on deuterated drugs have become more common. [6]
This is a list of fentanyl analogues (sometimes referred to as Fentalogs), [1] [2] [3] including both compounds developed by pharmaceutical companies for legitimate medical use, and those which have been sold as designer drugs and reported to national drug control agencies such as the DEA, or transnational agencies such as the EMCDDA and UNODC.
A 3-Dimensional (stick-&-ball) rendering of Troparil: A structural analogue of cocaine with omitted -COO- linkage – a parent compound of many MAT ligands; those of the phenyltropane class. (Here it is depicted in an unfavourable conformation of the O-Me; The methyl has to be at the other oxygen and trans to optimize its functional stimulation.)
The gabapentinoids are 3-substituted derivatives of GABA; hence, they are GABA analogues, as well as γ-amino acids. [ 3 ] [ 4 ] Specifically, pregabalin is ( S )-(+)-3-isobutyl-GABA, phenibut is 3-phenyl-GABA, [ 31 ] and gabapentin is a derivative of GABA with a cyclohexane ring at the 3 position (or, somewhat inappropriately named, 3 ...
(Reuters) -U.S. President-elect Donald Trump's transition team is exploring ways to significantly reduce, merge, or even eliminate the top bank regulators in Washington, the Wall Street Journal ...
Fewer than 30 different analogs of PCP were reported as being used as a street drug during the 1970s and 1980s, mainly in the United States. [48] Only of a few of these compounds were widely used including rolicyclidine (PCPy), eticyclidine (PCE), and tenocyclidine (TCP). [48] Less common analogs include 3-HO-PCP, 3-MeO-PCMo, and 3-MeO-PCP.
3,14-Diacetyloxymorphone [1] is an opioid analgesic which has never been marketed. It is an acetyl derivative of oxymorphone.It is related to other acetylated morphone derivatives, including 3,6-diacetyloxymorphone, 3,8,14-triacetyloxymorphone, 3,6,8,14-tetraacetyloxymorphone, noroxymorphone analogs of all or most of the above, and 3,6,14-triacetyloxymorphone, a derivative of oxymorphone whose ...