JNJ-10397049 is a potent and selective antagonist of the orexin-2 receptor. JNJ-10397049 regulated ovulation, and sleep promotion. JNJ-10397049 was reported to be effective in reducing the reinforcing effects of ethanol.

JNJ-10181457 is a histamine H3 receptor antagonist, which was developed by Johnson & Johnson. Selective blockade of histamine H3 receptors might have therapeutic utility for the treatment of working memory deficits and learning disorders, especially those in which ACh neurotransmission is compromised.

L-701,324 [7-chloro-4-hydroxy-3(3-phenoxy) phenylquinoline-2-(H)-one] is a selective and full antagonist at the glycine site of the NMDA receptor, has been studied on animals as potential antipsychotic and anticonvulsant agent. But these studies were discontinued.

1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea (A-425619), a novel, potent, and selective transient receptor potential type V1 (TRPV1) antagonist, attenuates pain associated with inflammation and tissue injury in rats. A-425619 was found to potently block capsaicin-evoked increases in intracellular calcium concentrations in HEK293 cells expressing recombinant human TRPV1 receptors (IC50 = 5 nM). A-425619 showed similar potency (IC50 = 3-4 nM) to block TRPV1 receptor activation by anandamide and N-arachidonoyl-dopamine. Electrophysiological experiments showed that A-425619 also potently blocked the activation of native TRPV1 channels in rat dorsal root ganglion neurons (IC50 = 9 nM). In vivo, A-425619 dose dependently reduced capsaicin-induced mechanical hyperalgesia (ED50 = 45 umol/kg p.o.). A-425619 was also effective in models of inflammatory pain and postoperative pain. A-425619 potently reduced complete Freund's adjuvant-induced chronic inflammatory pain after oral administration (ED50 = 40 umol/kg p.o.) and was also effective after either i.t. administration or local injection into the inflamed paw. Furthermore, A-425619 maintained efficacy in the postoperative pain model after twice daily dosing p.o. for 5 days. A-425619 also showed partial efficacy in models of neuropathic pain. A-425619 did not alter motor performance at the highest dose tested (300 micromol/kg p.o.). A-425619, a potent and selective antagonist of TRPV1 receptors, effectively relieves acute and chronic inflammatory pain and postoperative pain.

1,12-Dodecanediamine (Dytek-12) is a 12 carbon aliphatic diamine. It is a highly versatile polymer monomer and chemical intermediate that is useful in the manufacture of a variety of products.

AMD8664 (1-pyridin-2-yl-N-[4-(1,4,7-triazacyclotetradecan-4- ylmethyl)benzyl]methanamine) is an antagonist of CXCR4 receptor. It has therapeutic potential in the treatment of HIV. AMD8664 is an effective suppressor of choroidal neovascularization.

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.

LY-320135 is a substituted benzofuran which is structurally distinct from the aminoalkylindole and pyrazole type cannabinoid antagonists, AM630 and SR141716A, respectively. LY-320135 is a potent and selective canniboid CB1 receptor antagonist/inverse agonist. LY-320135 is selective (~70 fold) over canniboid CB2 receptors. LY-320135 is widely used in research, particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses. LY-320135 shows weak binding to both 5-HT2 (Ki = 6.4 uM) and muscarinic receptors (Ki = 2.1 uM).