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Restrict the search for
cocaine
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
L-152804 is a nonpeptide, potent, selective and orally available antagonist of a neuropeptide-Y Y5 receptor (NPY Y5). L-152,804 may attenuate drug-induced behavioral effects in vivo. L-152,804 prominently decreased nose-poking for the peak dose of cocaine and shifted the dose-response curve for cocaine downward in self-administration animal model of cocaine addiction-related behavior. Cocaine failed to increase c-fos expression in the nucleus accumbens and striatum of L-152,804-treated mice, indicating that the Y5 antagonist could act by influencing neural activity in these regions. Accordingly, the cocaine-induced increase in accumbal extracellular dopamine was attenuated by L- 152,804 and in Y5-KO mice, suggesting that Y5 antagonism influences cocaine-induced behavior by regulating dopamine. L-152,804 significantly reduced both the dosage of self-administered ethanol and the total number of ethanol-reinforced responses in a rodent genetic animal model of alcoholism. The most likely mechanism by which L-152,804 might have decreased g/kg ethanol intake in both behavioral models is by attenuation of its reinforcing properties. This was evidenced by reduced ethanol-reinforced responding in the absence of changes in response onset, which suggests that the NPY Y5 antagonist did not alter neurobiological processes that control the onset of ethanol responding but inhibited responding once it was initiated.
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
5-(2-Aminopropyl)indole (5-API, 5-IT, PAL-571) is a psychoactive phenethylamine derivative with empathogenic effects used for recreational purposes. 5-(2-Aminopropyl)indole, originally synthesized as a stimulant in the 1960s now joins the list of psychoactive substances and may to be one of the newest MDMA replacements. 5-(2-Aminopropyl)indole acts as a triple monoamine releasing agent and also as selective MAO-A inhibitor.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
LY235959 is the active isomer of the 6-substituted decahydroisoquinoline-3-carboxylic acid, LY274614. Both LY274614 and LY235959 have demonstrated potent NMDA receptor antagonist activity both in vivo and in-vitro. LY235959 has been shown to attenuate and reverse morphine tolerance as well as, attenuate opioid withdrawal and block c-fos mRNA induction in limbic areas. The attenuation of morphine tolerance occurs through the interaction of LY235959 with the NMDA receptor and not by producing opiate receptor changes. LY235959 is able to block NMDA receptor-induced hyperalgesia, as well as formalin-induced inflammatory pain, in rats. These antinociceptive effects of LY235959 were obtained at doses that did not produce motor impairment. LY235959 does not block the hyperalgesia produced by kainic acid (a non-NMDA glutamate receptor agonist) providing evidence of its selectivity for the NMDA receptor.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
GBR-12935 (1-{2-benzhydryloxyethyl}-4-(3-phenylpropyl)piperazine) is a potent and selective inhibitor of dopamine transporter. Gist-Brocades originally initiated studies of GBR-12935 for the treatment of cocaine dependence.
Tritium-labeled GBR-12935 may be used in radioligand binding studies. GBR-12935 is considered to be the metabolite of vanoxerine, another piperazine dopamine uptake inhibitor.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
SCH-442416 is a selective antagonist of the adenosine A2a receptor with a Ki of 0.48 nM. It was first designed and developed as an [11C] radioisotope for PET imaging and has seen some use as an investigational and diagnostic tool, including one human study (see: SCH-442416 C-11). The non-radiolabeled compound has garnered less interest. SCH-442416 has been investigated in rats as a treatment for learned cocaine addiction; However, another study in rats indicates that SCH-442416 upregulates expression of glutamate synthase (GS) and glutamate aspartate transporter (GAST) in Muller Cells which can exacerbate conditions such as Ocular Hypertension.
