Nalmefene Morphine receptor (inverseaRonisti receptor (full agonist) chloride in
ID: 239276 • Letter: N
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Nalmefene Morphine receptor (inverseaRonisti receptor (full agonist) chloride influx chloride influx treat opioid dependence pain centrally Respiration centrally Gastric motility locally opioid withdrawal Buprenorphine receptor (partial agonist) Chloride influx rabbits were given pentobarbital again; compared with naive rabbits, the pre-exposed rabbits had a shorter and slept for a shorter period, although plasma concentration when both group of rabbits woke up was comparable. This observation can be explained by A. Pharmacokinetic tolerance B pharmacodynamic tolerance C. Tachyphylaxis For the following questions, bubble in A if true, or B if false. 48. Investigational New Drug Applications (IND) require clinical investigations before filing with FDA 49.When you have "spare" receptors, EC50 KD 50.The beta adrenergic receptor is a G protein coupled receptor 51. A greater proportion of Caucasian have a form of the beta 1 adrenergic receptor with 0 higher activity (than Africans). Their hypertension may respond better to propranolol 2Explanation / Answer
48. Investigational new drug applications require clinical investigations before filing with FDA
FDA approves new drugs for sale in the US after NDA application is made by drug sponsors. The information gathered in the clinical trials of an IND will become a part of the NDA.
There are 3 IND types:
An investigator IND:
Submitted by the physician, who leads the investigation or clinical trial.
Emergency use IND: Allows the use of emergency drugs in critical situations
Treatment IND: Use of experimental drugs which shows effectiveness in clinical trials
There are two IND categories:
· Commercial
· Research (non-commercial)
The IND application must contain information in three broad areas:
· Animal Pharmacology and Toxicology Studies
· Manufacturing Information
· Clinical Protocols and Investigator Information
49. When you have “spare” EC50 >KD
EC50: Half maximal effective concentration (EC50)
It is the concentration of a drug, antibody or toxicant which induces a response halfway between the baseline and maximum after a specified exposure time. It is used as a measure of a drug's potency.
KD = dissociation CONSTANT.
1. KD is the concentration at which 50% of binding sites (receptors) are occupied by drug. 2. KD (dissociation constant) is the inverse of the drug affinity to the binding site ( affinity = 1 / KD )
EC50 for an agonist is less likely to be equal to its Kd because of the spare receptors are not so common. There is no predictable relationship between EC50 and Kd for specific agonist- receptor combination.
50. The beta-adrenergic receptor is a G protein-coupled receptor
The beta-adrenergic receptor is a G protein-coupled receptor that binds the catecholamines, epinephrine and nor-epinephrine. After stimulation of receptor, the activated G aids the stimulation of adenylyl cyclase and generation of cAMP which helps in the physiologic action of beta 2 receptor activation.
51. A greater proportion of Caucasians have a form of the Beta 1 adrenergic receptor with higher activity (than Africans). Their hypertension may respond better to propranolol.
Genetic and unidentified factors support the ethnic differences in the effectiveness of beta 2 blockers.
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