Table 1.
Application of different types of drugs on GPCRs.
| S. No | Targets/Name of receptor | Disease-associated | Mechanism of action | Name of drug | Manufacturer | Status |
|---|---|---|---|---|---|---|
| Anti-diabetic Drugs | ||||||
| 1. | AMY 1-3 | Type 1& 2 diabetes | Peptide agonist | Pramlintide | BMS/Amylin | Market |
| 2. | GLP-1 & GIP | Type 2 diabetes | Competitively inhibit DPP-4 | Sitagliptin (Januvia) | Merck & Co | Market |
| 3. | GLP-1 | Type-2 diabetes | Peptide agonist | Albiglutide | GSK | Market |
| 4. | GLP-2 | Type 2 diabetes | Peptide agonist | Teduglutide | NPS Allelix | Market |
| 5. | Prostanoid receptor | Ischemic stroke, pain, inflammation | Irreversibly acetylate Ser530 of COX-1, inhibits the generation of thromboxane A2 | Aspirin | Bayer Bitterfeld GmbH Germany | Market |
| 6. | Protease activated receptor-1 (PAR-1) | Myocardial infarction, coronary revascularization | Inhibits thrombin related platelet aggregation | Vorapaxar (Zontivity) | Merck and Co. | Market |
| Anti-platelet & Cardiac Drugs | ||||||
| 7. | P2Y12 | Acute coronary syndrome, peripheral artery disease | Selectively inhibits the binding of ADP to P2Y12 | Clopidogrel (Plavix) | Bristol-Myers-Squibb-Sanofi | Market |
| 8. | P2Y12 | Stent thrombosis & myocardial infarction | Blocks ADP-induced platelet activation and aggregation | Cangrelor (Kangreal) | Parsippanny | Market |
| 9. | A2A Adenosine receptor | Coronary vasodilator | Elevated coronary flow reserve via selective A2A receptor activation | Regadenoson (Lexiscan) | Astellas Pharma | Market |
| 10. | α-2 Adrenergic receptors | Myocardial ischemia, clinical anesthesia | Neuronal hyperpolarization | Dexmedetomidine (Precedex) | Pfizer | Market |
| 11. | Beta adrenergic receptor | Myocardial infarction, hypertension | Function as beta 1 receptor antagonists | Acebutolol (Sectral) | Sanofi Aventis | Sanofi Aventis |
| Miscellaneous drugs acting on different types of receptors | ||||||
| 12. | CTR | Osteoporosis, hypercalcemia, Paget’s hemiplegia | Acts primarily on bone | Calcitonin- Salmon | Novartis | Market |
| 13. | CGRP | Migraine | CGRP receptor mab | Galcanezumab (LY2951742) | Eli Lilly | Phase III |
| 14. | GHRH | HIV-associated lipodystrophy | Peptide agonist | Tesamorelin | Theratechnologies Inc | Market |
| 15. | PTH1 | Osteoporosis | Peptide agonist | Teriparatide | Eli Lilly | Market |
| 16. | CXCR4 | Cancer | Mobilizes hematopoietic stem cells | Plerixafor (Mozobil) | AnorMED/Genzyme | Market |
| 17. | α-1 Adrenergic receptors | Epistaxis, Drooping eyelids | Vasoconstrictor and targets subset of adrenoreceptors in Muller’s muscle of the eyelid | Oxymetazoline (Afrin, Otrivin) | Merck | Market |
| 18. | β-3 Adrenergic receptor | Overactive bladder | Relaxes detrusor smooth muscle | Mirabegron (Myrbetriq) | Astellas Pharma Inc | Market |
| 19. | AT1 receptor antagonists | High blood pressure, congestive heart problem | Selectively block the binding of angiotensin II to AT1 | Candesartan (Atacand) | AstraZeneca, Takeda Pharmaceuticals | Market |
| 20. | Bradykinin B2 receptor antagonist | Hereditary angioedema | Elevates vessel permeability dilates blood vessel and contracts smooth muscle cells | Icatibant (Firazr) | Shire Plc | Market |
| 21. | Calcium sensing receptor | Chronic kidney disease | Allosteric activator of the parathyroid gland | Etelcalcetide (Parsabiv) | Amgen | Market |
| 22. | MT1 and MT2 receptor | Insomnia and sleep disorders | Inhibits neuronal firing | Ramelteon (Rozerem) | Zydus Cadila | Market |
| 23. | NTS2 receptor | Conjunctivitis | Prevents histamine binding and activity | Levocabastine (Livostin) | Janssen Pharmaceutica | Market |
| 24. | Mu-opioid receptor | Primarily used for local anesthesia in surgery | Inhibits the release of numerous neurotransmitters | Alfentanil (Alfenta) | Janssen Pharmaceutica | Market |
| 25. | Prostaglandin E1 receptor | Stomach ulcer, postpartum bleeding | Inhibits basic & nocturnal gastric acid secretion | Misoprostol (Cytotec) | Pfizer | Market |
| 26. | Prostaglandin F receptor | Ocular hypertension, open-angle glaucoma | Increases outflow of aqueous humor | Latanoprost (Xalatan) | Pfizer | Market |
| Neurological drugs | ||||||
| 27. | GPR143 receptor | Parkinson disease | DOPA decarboxylase converts levodopa to dopamine | Levodopa | Sandoz | Market |
| 28. | Muscarinic acetylcholine receptor | Alzheimer’s disease | Donepezil reversibly inactivates the cholinesterase | Donepezil (Aricept) | Pfizer | Market |
| 29. | Serotonin 1A (5-HT1A) receptor | Schizophrenia, Bipolar disorder | Aripiprazole is a partial HT1A agonist | Aripiprazole (Abilify) | Bristol-Myers Squibb | Market |
| 30. | Kainate & NMDA receptor | Amyotrophic lateral sclerosis | Directly inhibit kainite and NMDA receptor | Riluzole (Rilutek) | Sanofi Aventis | Market |
| 31. | 5-HT3 receptor | Epilepsy | Repress the release of glutamate & aspartate in the CNS | Lamotrigine (Lamictal) | GlaxoSmithKline | Market |