A5069206468- Neuropeptides and Animal Physiology
- Pharmacological Effects and Assays
- Receptor Mechanisms and Signaling
- Pain Mechanisms and Treatments
- Cancer, Stress, Anesthesia, and Immune Response
- Pharmacological Receptor Mechanisms and Effects
- Pulmonary Hypertension Research and Treatments
- Nicotinic Acetylcholine Receptors Study
- Marine Sponges and Natural Products
Dominican University of California
2015-2018
Opioid therapeutics are excellent analgesics, whose utility is compromised by dependence. Morphine (1) and its clinically relevant derivatives such as OxyContin (2), Vicodin (3), Dilaudid (4) "biased" agonists at the μ opioid receptor (OR), wherein they engage G protein signaling but poorly β-arrestin endocytic machinery. In contrast, endorphins, endogenous peptide for ORs, potent show reduced liability tolerance dependence, both pathways "balanced" agonists. We set out to determine if...
Opioid receptors belong to the large superfamily of seven transmembrane-spanning (7TM) G protein-coupled (GPCRs). As a class, GPCRs are fundamental physiological importance mediating actions majority known neurotransmitters and hormones. The Mu, Delta, Kappa (MOP, DOP, KOP) opioid particularly intriguing members this receptor family as they targets involved in many neurobiological diseases such addiction, pain, stress, anxiety, depression. Recently we discovered that aaptamine class marine...
Opioid receptors belong to the large superfamily of seven transmembrane-spanning (7TM) G protein-coupled (GPCRs). As a class, GPCRs are fundamental physiological importance mediating actions majority known neurotransmitters and hormones. The Mu (µ), Delta (δ) Kappa (MOR, DOR, KOR) opioid particularly intriguing members this receptor family as they targets involved in many neurobiological diseases such addiction, pain, stress, anxiety, depression. To date few marine natural products have been...
Recently we discovered that the aaptamine class of marine sponge derived natural products exhibit selective agonist activity in vitro for delta opioid receptor (DOR) versus mu (MOR). Our findings may explain reports by others (1) demonstrates vivo anti-depressant effects mouse models using Porsolt Forced Swim Test. This project involved extraction Aaptos aaptos (a source 1), establishing a scale up purification procedure to provide sufficient amounts 1 (30 mg) follow evaluation and...