CLOSE MENU

HOME

TEST SERIES

GPAT

NIPER

DRUG INSPECTOR

PHARMACIST

JOBS

SEARCH JOBS

POST YOUR JOB

PHARMA INFO PARK

SCHOLARSHIP

ADMISSION ALERTS

AWARDS AND SCHOLARSHIPS

CAREER COUNSELING

EDUCATION LOAN

FUNDING AGENCIES AND GRANTS FOR RESEARCH

HOW TO PREPARE FOR GPAT

JOB ALERTS

PHARMA COMPANY

PHARMA EXPERIMENTS

PHARMA NEWS

SCHOLARSHIP ALERTS FOR PHARMACY

SOPS FOR SCIENTIFIC INSTRUMENTS

STUDY MATERIAL

SUCCESSFULL GPAT INDIAN

TRAINING OPPORTUNITIES FOR PHARMACY PROFESSIONALS

TRAVEL GRANT

CONFERENCE

SEARCH CONFERENCE

POST YOUR CONFERNCE

MOCK TESTS

GPAT MOCK TEST

NIPERJEE MOCK TEST

PHARMACIST MOCK TEST

DRUG INSPECTOR MOCK TEST

UGC NET MOCK TEST

GATE MOCK TEST

EXAMS

GPAT

NIP

NHENINDAMINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses

PHENINDAMINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses

 October 23, 2020  huzefakifayet GATE Exam, GPAT Preparation, How to prepare for gpat, MCQ, Medicinal Chemistry, NEET PG, NEET UG, NIPER JEE Examination (Masters/Ph.D. Admission), Pharmacy Exam Questions, Quiz, Study Material, UGC NET JRF Exam CSIR MCQ PHENINDAMINE solved, DBE BET MCQ PHENINDAMINE solved, Drug inspector PHENINDAMINE solved, GATE MCQ PHENINDAMINE solved, GPAT MCQ PHENINDAMINE solved, gpatindia, NIPER MCQ PHENINDAMINE solved, Pharmacist MCQ PHENINDAMINE solved, PHENINDAMINE, PHENINDAMINE chemical properties, PHENINDAMINE gpat questions, PHENINDAMINE gpatindia, PHENINDAMINE mechanism of action, PHENINDAMINE MEDICINAL CHEMISTRY, PHENINDAMINE MELTING POINT, PHENINDAMINE MOLECULAR WEIGHT, PHENINDAMINE NUMBER OF CHIRAL CARBONS, PHENINDAMINE OCTANOL WATER COEFFICIENT, PHENINDAMINE physical properties, PHENINDAMINE RING STRUCTURE, PHENINDAMINE SAR, PHENINDAMINE side effects, PHENINDAMINE SOLUBILITY, PHENINDAMINE structure, PHENINDAMINE synthesis, PHENINDAMINE therapeutic uses, staff nurse MCQ PHENINDAMINE solved

 


Phenindamine           

 

IUPAC nomenclature


2-methyl-9-phenyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine




 


Classification

H1-receptor antihistamine

Alkylamine antihistamine

 


Physiochemical Properties

S. NO. PHYSICAL AND CHEMICAL PROPERTIES

1 Molecular weight 261.4 g/mol

2 Physical appearance Solid

3 Melting point 91oC

4 Solubility 2.77e-02 g/L

5 Octanol/water partition coefficient N/A

5 Presence of ring Indenopyridine, phenyl

6 Number of chiral centers 1

 


Mechanism of Action

Phenindamine competes with histamine for binding with H1 receptor site on the effector cell.

Thus, all those pharmacological responses which were mediated by histamine at H1-receptor site are reduced and the intensity of allergic reactions and tissue injury response involving histamine release are reduced.

 

Structure Activity Relationship

Structure activity of alkyl amines antihistamines can be summarized as:


E- and Z- isomers in alkenes shows large difference in activity, where, E-isomers are more potent than Z-isomers.

The two aromatic rings have different binding environments at the receptors.

5-6 angstrom distance is required between aromatic ring and tertiary aliphatic amine for biding at the receptor.

S­-enantiomers have greater affinity for H1 histamine receptors [1]

 

Method of synthesis

Acetophenone, methylamine and formaldehyde are reacted together to get ß,ß’-(methylamino)bis-(propiophenone).

The above formed compound is treated with sodium hydroxide to get 3-benzoyl-4-hydroxy-1-methyl-4-phenyl-piperidine.

On reaction of last with concentrated hydrogen bromide, 2-methyl-9-phenyl-2,3-dihydro-1H-indeno[2,1-c]pyridine is formed.

The last is reduced to get phenindamine. [2]



Medicinal Uses

Phenindamine is used for treatment of:


Allergies

Hay fever

Common cold

Watery eyes

Runny nose

Sneezing

 


Side Effects

Side effects of Phenindamine are:


Fatigue

Dizziness

Drowsiness

Sleepiness

Dry mouth

Enlarged prostate

Difficulty in urination

Headache

Difficulty breathing

Closing of throat

Swellings in face

 


MCQs

Q.1 Match the following with correct SAR of the alkylamines antihistamine drugs:


i. E-isomers are A. More potent than Z-isomers

ii. S-enantiomers have B. Less potent than Z-isomers

  C. Greater affinity for H1-receptors

  D. Greater affinity for H2-receptors

i-A, ii-C

i-A, ii-D

i-B, ii-C

i-B, ii-D

Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?


Phenindamine: 2-methyl-9-phenyl-2,3,4,9-tetrahydro-1H-indeno[2,1-c]pyridine

 Diphenhydramine: 2-(diphenylmethoxy)-N,N-dimethylethanamine

 Auranofin: gold(1+);3,4,5-triacetyloxy-6-(acetyloxymethyl)oxane-2-thiolate;triethylphosphanium

 Meloxicam: 4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-1,1-dioxo-1λ6,2-benzothiazine-3-carboxamide

a) TFFT


b) FFTF


c) TTTT


d) FFFT


Q.3 Molecular weight of Phenindamine is?


a) 200.5 gm/mol


b) 540.6 gm/mol


c) 261.4 gm/mol


d) 1042 gm/mol


Q.4 Phenindamine binds with which receptor to produce antihistaminic actions?


a) α-receptors


b) ß-receptors


c) Nicotinic receptor


d) H1-receptor


Q.5 Which amongst the following is not a therapeutic use of drug phenindamine?


a) Runny nose


b) Sneezing


c) Hay fever


d) Hypertension


Q.6 Which of the following drug and their classification are correct?


I. Phenindamine: H1 receptor antihistamine drug


II. Cimetidine: H2 receptor antihistamine drug


III. Lansoprazole: Proton pump inhibitor


IV. Thiotepa: Antineoplastic drug


a) I, III


b) I, II, III, IV


c) III, IV


d) I, II, IV


Q.7 Number of chiral centers present in the structure of phenindamine is?


a) 0


b) 1


c) 2


d) 3


 


 


Comments

Post a Comment

Popular posts from this blog

Only remember

 Sikho English With Hindi (daily used english sentences,uses, learn spoken english, SSC, railway, banking & competitive exams): Eerie:भयानक Enmesh:जाल में फंसना Sob:सिसकी Tatter:फटे कपड़े My mobile was out of order. That's why I was not able to post contents. Notorious:- A man with evil reputation (एक बदनाम व्यक्ति) रोहन विश्वास मत करो। वह एक बदनाम वयक्ति है। Don't trust Rohan. He is a notorious. Cowranch:गौशाला Enisles:पृथक करना Elaborative:विस्तार Acrobats:कलाबाज़ (01) Lightening (हल्का करना) He is lightening my burden. वह मेरे बोझ को हल्का कर रहा है। (02) Lightning (बिजली चमकना) Last night there was flash of lightning in the sky. पिछली रात आसमान में बिजली कड़की (03) Lighting (प्रकाश व्यवस्था) There was good lighting arrangement at the marriage. विवाह के अवसर पर प्रकाश व्यवस्था अच्छी थी। (01) Affect (प्रभावित करना) Your behaviour should affect others. तुम्हारा व्यवहार दूसरों को प्रभावित करना चाहिए। (02) Effect (प्रभाव) His speech didn't produce any effect on the audie...
Read more

vit d3

Vitamin A : 1 IU is the biological equivalent of 0.3 mcg retinol, or of 0.6 mcg beta-carotene Vitamin C : 1 IU is 50 mcg L-ascorbic acid Vitamin D : 1 IU is the biological equivalent of 0.025 mcg cholecalciferol or ergocalciferol Vitamin E : 1 IU is the biological equivalent of about 0.67 mg d-alpha-tocopherol, or 0.9 mg of dl-alpha-tocopherol. Example conversion Let's say that I have a soft gel capsule that contains 500 IU of Vitamin A as retinol. To convert this to mcg, using the information above, I would multiply it by 0.3: 500 × 0.3 = 150mcg. Conversely, if the soft gel capsule was described as '150mcg of Vitamin A as retinol' and I wanted to convert to IU, I would divide it by 0.3. 150 ÷ 0.3 = 500 IU. Note that the information contained here is purely for casual interests and is not intended to replace your doctor's advice. Please use it at your own risk. As with all calculations where health could suffer from inaccurate conversions, ...
Read more