Cannabinoids and the ECS

The word cannabinoid refers to molecules that interact with cannabinoid receptors. Cannabinoids are produced naturally by human beings (endocannabinoids), all other mammals, and by plants (phytocannabinoids pCBs).

The cannabis plant produces over 100 active phytocannabinoids. The two best known cannabinoids are delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD). The most widely recognised is THC, the compound that is primarily responsible for the psychoactive effects of cannabis. However, a recent increase in the use of cannabis extracts has resulted in the growing popularity of CBD.  At OCT, we are focused on 3 types of cannabinoids:  synthezised phytocannabinoids (pCBs), cannabinoid derivatives and novel chemical entities (NCEs) which are not cannabinoids but behave like them.

The Endocannabinoid System

Science has shown us that a key biological system in the human body, The Endocannabinoid System (ECS), plays an important role in maintaining the balance between our physical and mental health including regulating pain, mood, memory, sleep, appetite, and the immune response to cancer. 

ECS receptors are found in the brain and peripheral nervous system, but also in many other cells throughout the body. The most studied and prominent are the CB1 and CB2 receptors.

Through medicinal chemistry and screening, cannabinoid derivatives and other new chemical entities can be designed to target single receptors. OCT461201, for example, is highly selective for CB2. Targeting CB2 has many benefits, including anti-neuroinflammatory and nociceptive properties, without any psychoactive side-effects. OCT130401 combines two different cannabinoids which are known for their analgesic and anti-inflammatory properties. The combination aims to provide both immediate pain relief and long-term amelioration of the painful conditions where inflammation plays a role.

CB1 receptors

  • Primarily found in neuronal cells; also in peripheral organs and tissue

  • CB1 modulation impacts pain, motor control, memory & behaviour

  • CB1 mediates psychoactivity

CB2 receptors

  • Primarily expressed in immune cells & lymphoid organs; lungs; heart; bones; gastrointestinal and liver

  • Receptor stimulation does not produce psychoactive effects

  • CB2 agonists appeal as therapeutics in auto-immunity; inflammatory disorders; chronic pain and cancer