Our Research
CB1 & CB2
Recent scientific discoveries have shown that the human body produces endogenous cannabinoids (endocannabinoids), a family of neurotransmitters and neuromodulators. These natural substances participate in a number of physiological processes by interacting with two known cannabinoid receptors (CB1 and CB2) as well as a group of enzymes and a transporter system all of which serve as potential targets for drug discovery. Cannabis has been recognized to have therapeutic effects since ancient times and has been used as an analgesic, an appetite enhancer and in combating nausea and vomiting but has not been fully exploited as a therapeutic agent because of its undesirable mood altering effects. MAKScientific’s technology provides an excellent opportunity to create novel and highly effective medications without the undesirable psychotropic side effects associated with cannabis. The company has synthesized compounds that are in pre-clinical development for the treatment of obesity, neuropathic, somatic and inflammatory pain, addiction, neuroprotection, and glaucoma. MAKScientific has highly developed tools and technologies that it employs in the course of its research in the areas of medicinal chemistry, molecular biology and molecular modeling. It has proprietary cell culture lines and has sophisticated biochemical and pharmacological assays as well as conducted tests on animal models to further drug discovery efforts.
MAKScientific has a library of over 5,000 compounds covering various therapeutic categories. Immediately after synthesis, purification and characterization, each compound is tested in vitro for its affinity for the cannabinoid receptors, its agonistic or antagonistic properties and its effects on the anandamide transporter and anandamide amidase. Based on the in vitro data generated, appropriate compounds are selected for efficacy studies in various animal models.
Obesity
It has been shown that CB1 receptor antagonists can block the craving for food and that appetite suppression is a viable mechanism for treating obesity. Rimonabant, a selective CB1 antagonist, has demonstrated effective weight reduction, metabolic risk factor improvement and a positive safety profile in Phase III studies. In additional studies in type II diabetes patients, the drug reduced blood glucose, lowered triglycerides and raised HDL (good cholesterol) levels.
MAKScientific has developed novel, bioavailable CB1 receptor antagonists with improved pharmacological profiles. The compounds are highly selective for the CB1 receptor, do not interact with the CB2 receptor and are expected to have fewer side effects than other drugs in development and exhibiting high affinity for the receptor. In rats, the compounds reduced food consumption, demonstrated very high oral bioavailability and excellent safety. These promising candidates have pharmacological profiles superior to those of other CB1 antagonists reported in the literature (including rimonabant).
Neuropathic Pain
A novel class of drugs, selective CB2 receptor agonists have demonstrated analgesic activity in preclinical animal models of nociceptive, inflammatory and neuropathic pain. Because this class of cannabinoid receptors is found outside the central nervious system, CB2 receptor agonists are anticipated to be devoid of the CNS side effects that are associated with non-specific and CB1 cannabinoid receptor agonists. If proven effective, the ability of these non-opioid compounds to treat pain of significant severity could establish a whole new class of analgesics with the potential to rival opioids in pain control.
Neuropathic pain results from a pathological abnormality in the nervous system itself. Treatment for the management of neuropathic pain is one of the greatest challenges facing today’s medical practice. Approximately 1.5% of the population (2.8 million people) in the United States suffers from moderate to severe neuropathic pain associated with back pain, diabetic neuropathy, carpal tunnel syndrome, complex regional pain syndrome, HIV/AIDS neuropathy, phantom limb pain, spinal cord injury, post-herpetic neuralgia, and trigeminal neuralgia. Unlike nociceptive pain, which is the process of pain transmission usually relating to a receptive neuron for painful sensations, neuropathic pain does not yield readily to standard treatment with anti-inflammatory drugs or to opoid therapy.