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Medicinal Chemistry
| Question | Answer |
|---|---|
| What is a conformational isomer? | Two compounds with the same chemical formula and structure but a different shape. Ex."boat" cyclohexane vs. "chair" cyclohexane |
| What is a structural isomer? | Two compounds with the same chemical formula but a different structure. Ex. n-propranol vs. isopropanol |
| What is a steroisomer? | Two compounds with the same chemical formula but different 3D arrangement of atoms. |
| What is chirality? | It is a property of a molecule whereby it has a nonsuperimposable mirror image |
| What is a racemic mixture? | A mixture containing EQUAL AMOUNTS of both stereoisomers of a molecule. |
| Screening using libraries are often used for (less well-understood/ well-understood) targets? | less well-understood targets, newly-discovered targets |
| Structure-based drug design is generally used for (less well-understood/ well-understood) targets. | well-understood targets |
| Ligand-based development is (classic/ genomic). | classic |
| Receptor-based development is (classic/ genomic). | genomic |
| (Classic/ genomic) has a potential for greater number of side effects and lower therapeutic index | classic |
| Any molecule which binds to an opioid receptor | opioid |
| A natural product, or semi-synthetic analog of a natural product, that is derived from opium and binds to an opioid receptor. | opiate |
| The dried sap collected from the opium poppy | Opium |
| Opium receptors are (GPCRs/ ligand-gated ion channels) | GPCRs |
| Opioid receptors couple to (Gq/Gs/Gi) | Gi, thus inhibiting adenylyl cyclase |
| What are the 3 opioid receptor subtypes? | mu, delta, kappa |
| Tolerance is an agonist effect of which opioid receptor (mu, delta, kappa)? | Mu |
| sedation is an agonist effect of which opioid receptor (mu, delta, kappa)? | Kappa |
| Dysphoria is an agonist effect of which opioid receptor (mu, delta, kappa)? | Kappa |
| Constipation is an agonist effect of which opioid receptor (mu, delta, kappa)? | Mu |
| Dependence is an agonist effect of which opioid receptor (mu, delta, kappa)? | Mu |
| Immune suppression is an agonist effect of which opioid receptor (mu, delta, kappa)? | Mu |
| Respiratory depression is an agonist effect of which opioid receptor (mu, delta, kappa)? | Mu and Delta |
| Miosis is an agonist effect of which opioid receptor (mu, delta, kappa)? | Kappa |
| Diuresis is an agonist effect of which opioid receptor (mu, delta, kappa)? | Kappa |
| Endorphin is an endogenous ligand for what type of opioid receptor (mu, delta, kappa)? | Mu, Delta, and Kappa |
| Enkephalin is an endogenous ligand for what type of opioid receptor (mu, delta, kappa)? | Mu and delta |
| Endomorphin is an endogenous ligand for what type of opioid receptor (mu, delta, kappa)? | Mu |
| Dynorphin is an endogenous ligand for what type of opioid receptor (mu, delta, kappa)? | Kappa |
| What is the most common mental illness? | depression |
| What are the on target effects of TCAs? | inhibition of brain norepinephrine and serotonin reuptake transporters. |
| What are the off target effects of TCAs? | inhibition of H1, alpha 1, and muscarinic receptors |
| What type of drug has a 6-7-6 ring structure? | TCAs |
| What is the molecular target of the barbiturate drug class? | GABA(A) receptors. They allosterically activate the ability of GABA to open the GABA(A) chloride channel. |
| What are the two important determinants of membrane permeability? | Ionizability and lipophilicity. (less ionizability= better absorption; greater lipophilicity= better absorption) |
| How is the absorption of barbiturates enhanced? | The C5 hydrogens are replaced with alkyl or aryl groups to lower ionizability. |
| What are the 3 things that lipophilicity directly affects? | blood-brain barrier penetration, absorption from GI tract, and metabolism |
| What is the partition coefficient (P)? | It is a measure of lipophilicity. Larger log P value = greater lipophilicity |
| Greater lipophilicity = (slower/quicker) onset = (shorter/longer) duration of action | quicker, shorter |
| What are the two ways to increase lipophilicity? | 1. by increasing the size of the R groups, 2. by replacement of oxygen with sulfur. |
| Why does greater lipopilicity lead to a shorter duration of action? | High lipophilicity can result in redistribution to fat-loving cells like adipose tissue. |
| What is the molecular target of the benzodiazepines? | They bind the GABA(A) receptor at the alpha1-6 and gamma2. |
| What is a Pharmacophore? | A structural framework illustrating the features shared by a set of molecules that bind the same target. |
| What is a Privileged structure? | A single molecular framework able to provide ligands for diverse receptors. "Key Template" It can be modified to bind many targets. |
| Active metabolites have a (shorter/longer) duration of action, while inactive metabolites have a (shorter/longer) duration of action. | longer, shorter |
Created by:
nanapack