Dopamine receptors can be affected by agonists, partial agonists, and antagonists. An agonist is a drug that causes an action when it binds to the receptor. It essentially tricks the receptor into believing that it is a neurotransmitter and causes the receptor to produce the same action that a real neurotransmitter would. Some examples of agonists are bromocriptine, cabergoline, pramipexole, ropirinole, and apomorphine. An antagonist is a drug…
the beginning of the concentration-response curve. EC50 of Ach is 7.47 x 10-7M whereas EC50 of 5-HT is 7.97 x 10-7M. The contraction generated by Ach and 5-HT was expressed in % Emax. As shown in Fig. 1 and 2, % Emax increased with increasing agonists concentrations and 100% Emax was achieved at a concentration of 30μM. Presence of error bars in both figures indicated the presence of variability in data. We then investigated the effect of Ach and 5-HT…
To understand the effects of agonists and competitive antagonists the receptors involved must be identified first. There are 2 major groups of receptors present in rat ileum, the first being 5-hydroxytryptamine (5-HT) receptors and the second, muscarinic acetylcholine receptors (mAChR) – and of these two groups there are certain subtypes in the ileum contributing to its tone, motility, secretion and blood flow. The 5-HT receptor subtypes most prevalent in the rat ileum were, 5-HT2A, 5-HT2B,…
that are capable of binding to receptors to inhibit the possession of agonists but do not have intrinsic activity. Receptor antagonists are divided into competitive antagonists and non-competitive antagonists (Rang et al., 2007). The second type is non-receptor antagonists that have two main approaches to prevent agonists. Chemical antagonists and physiologic antagonists are two kinds of non-receptor antagonists to inactive agonists (Golan et al., 2012). The classification of antagonists can see…
Albuterol is an adrenergic receptor agonist with pharmacological properties and therapeutic indications similar to terbutaline. The mechanism of the anti-asthmatic action of adrenergic receptor agonists is without a doubt linked to the direct relaxation of airway smooth muscle and the bronchodilator. Although human bronchial smooth muscle receives little or no sympathetic stoppage, it contains large numbers of adrenergic receptors. When the adrenergic receptors activate the adenylyl cyclase…
The Role of Alpha-1 Adrenergic Receptor in Disease Adrenergic receptors are a class of G-protein coupled receptors (GPCRs) which are activated by catecholamines in the central and peripheral nervous systems. Alpha-1 adrenergic receptors (1-AR) are systematic vasoconstrictors: their activation constricts blood vessels by the contraction of vascular smooth muscle. These transmembrane receptors are activated by the binding of epinephrine or norepinephrine, which creates intracellular signals via…
action, i.e., agonist or antagonist. Agonist drugs are those that copy the effects of naturally occurring neurotransmitters by facilitating postsynaptic activity. Within the agonist categorization there are two subtypes. First is direct-binding agonist, which binds directly to the receiving end of the synapse. This binding effect allows the individual to experience the drug similarly to it being released directly into the brain (New Health Guide, 2016). Second is indirect-acting agonist,…
hence also called the B10 cells. As this phenotype is identifies to regulate T cell dependent inflammatory response, they are researched for role in myasthenia gravis and other neuro inflammatory diseases. C. Terbutaline is a B2 adrenergic receptor agonist causing vasodilation, smooth muscle relaxation and skeletal muscle contractions.…
delta- and kappa-opioid receptors, thus inhibiting and modulating pain signals.88 Morphine is a pure mu-opioid receptor agonist with a great hypoalgesic effect and very used in veterinary medicine.89 Since pure mu-agonist opioids cause addiction in humans, the use of these opioids is strictly controlled, which may limit their use. Butorphanol is a kappa-opioid receptor agonist and a mu-antagonist, which limits its analgesic properties and efficacy.89 Buprenorphine is a partial mu-opioid receptor…
1. What clinical findings are likely in R.S. as a consequence of his COPD B? There are multiple types of chronic obstructive pulmonary disease (COPD), COPD “characterized by chronic and recurrent obstruction of airflow in the pulmonary airways (Porth & Matfin, 2009). The recurrent obstruction makes it difficult for a person to breath overtime this problem occurs in the lower respiratory tract. COPD compromises the flow of air in the lungs this causes less oxygen that is being circulated…