An Agonist-To-Antagonist Spectrum of Action and How Partial and Inverse Agonists Influence Psychopharmacologic

 

An antagonist binds at the receptors by blocking any event of an agonist, hence, blocking the biological response. For example, naloxone is a competitive opioid antagonist and has no effects with opioid co-administration (Gicquelais, et al, 2019). An agonist binds to a receptor causing activation of the receptor, hence, the biological response. A partial agonist activates the receptors partially with lesser effect on the brain. For example, buprenorphine is a partial agonist, and therefore, an antagonist may block its opioid function without activating its receptors. An inverse receptor binds with constitutively active receptors and inhibits receptor activity by exerting opposite pharmacological effects that suppress spontaneous receptor signaling.

Comparison between Actions of G Couple Proteins and Ion Gated Channels

G coupled proteins GPCRs are integral membrane proteins that convert extracellular responses to hormones, neurotransmitters, olfaction, and taste signals. The GPCRs work by binding to the hormones, neurotransmitters, and growth factors to initiate a cellular response. The three types of G-couple receptors are alpha, beta, and gamma, in which the ligands bind and activate (Yudin & Rohacs 2019). Ion gated channels are integral membrane proteins of excitable cells that allow a flux of ions to pass only under defined circumstances. These channels are voltage-gated sodium channel neurons and ligand-dated acetylcholine receptors of the cholinergic synapses. The ion gated channel pull and bonds to the agonist changing the protein while g coupled proteins are used by the cells to convert intracellular signals into responses.

The Role of Epigenetics In the Pharmacologic Action

Epigenetics regulate gene activity by switching off the gene activity or activating the gene activity. Epigenetics plays a role in the phenotypic activity of the cell in diseases such as cancer and neurodegenerative disorders such as Alzheimer’s disease. Epigenetics modify gene expressions after drug administration to counteract the disease states in humans. Epigenetics proves its effectiveness in treating psychiatric and neurodegenerative disorders to its ability to modify gene expressions.

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